巻号一覧
57 巻, 4 号
選択された号の論文の23件中1～23を表示しています
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Regular Articles
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Tomohiro Hamashita, Tetsuo Ono, Masaki Ono, Yoshinobu Tsunenari, Takao ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 325-331
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe preparation of core particles suitable for subsequent film coating was examined using different scales of agitation fluidized beds. Specifically, the effects of agitator rotational speed and agitator blade shape in different scales of granulators on granule properties such as mass median diameter, apparent density, friability and shape factor were studied. As the agitator rotational speed was increased or when the agitator blade height and angle were large, the mass median diameter and friability of the granules decreased, while the apparent density and shape factor increased, in a manner independent of the vessel size because the granules were subjected to greater compression, shearing and rolling effects. The same core particles could not be prepared using granulators with different vessel sizes by simply adopting a conventional scale-up theory1,2) based on kinetic energy similarity. Here, a novel scale-up theory that takes into account agitator blade shape factors is proposed.3) When the two scale-up theories were compared, our new theory was capable of predicting the granule properties more accurately than the conventional theory. By adopting this novel theory, the same core particles could be prepared under different operating conditions in any scale of granulator.抄録全体を表示PDF形式でダウンロード (397K) -
Naoko Katsuma, Yuki Sato, Kazuhiro Ohki, Keiko Okimura, Kuniharu Ohnis ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 332-336
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーTwelve N-terminal analogs of des-fatty acyl-polymyxin B (Des-FA-[X1]-PMB, X=various amino acids or peptides) were synthesized and examined for their antimicrobial activity against Escherichia coli (E. coli), Salmonella Typhimurium (S. Typhimurium) and Pseudomonas aeruginosa (P. aeruginosa). It was found that Des-FA-[Dap1]-, Des-FA-[Ser1]-, Des-FA-[Dab-Dab-Dab1]- and Des-FA-[Arg-Arg-Arg1]-PMB had potent activity only against P. aeruginosa, with MIC values of 0.5—1 nmol/ml. Analogs in which X was Lys, Arg, Leu or Ala did not have increased antimicrobial activity against the three bacterial species tested compared with the lead compounds Des-FA-[Dab1]-PMB and polymyxin B (PMB). Des-FA-[Trp1]-PMB and Des-FA-[Phe1]-PMB had reduced activity against P. aeruginosa. The results indicate that compact hydrophilic amino acids (C3) or basic tripeptides at the N-terminal provide specificity for bactericidal activity towards P. aeruginosa. For LPS-binding activity, Des-FA-[Dab-Dab-Dab1]-PMB and Des-FA-[Arg-Arg-Arg1]-PMB showed activity comparable to PMB, while Des-FA-[Ala-Ala-Ala1]-PMB showed very low activity. Reduced acute toxicity of Des-FA-[Dap1]-PMB and Des-FA-[Trp1]-PMB was demonstrated by a mouse tail intravenous administration test, with LD50 values of 23.5 and 19.0 μmol/kg, respectively, in contrast to PMB (LD50, 4.8 μmol/kg).抄録全体を表示PDF形式でダウンロード (172K) -
Dali Shukla, Subhashis Chakraborty, Sanjay Singh, Brahmeshwar Mishra原稿種別: Regular Article
2009 年 57 巻 4 号 p. 337-345
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe present investigation was undertaken to design a simple, rapid, cost effective and highly efficient process to fabricate a tasteless complex of risperidone using ion exchange resin (IER), evaluate the molecular properties of the resinate and finally incorporate it into orally disintegrating tablets (ODT). The resinate formation using Amberlite IRP64, was confirmed using the characterization methods: Fourier transform-infrared (FT-IR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The maximum loading efficiency achieved was 99.72±0.16% in 1 : 4 (drug : resin weight) ratio at pH 6.0, temperature at 22 °C in a period of 1.5 h using ethanol : water (1 : 1, v/v) as the complexation medium. The complex was compressed into orally disintegrating tablet. The drug release from the complex was about 2.5% in 120 s in 5 ml of pH 6.8 phosphate buffer which has been used to mimic the salivary fluid volume and pH. Dissolution studies using 500 ml of 0.1 N HCl at 50 rpm in USP Apparatus II released 92% in 5 min, indicating complete drug release from the complex in the stomach. Resinate was tasteless while the fabricated ODTs were pleasantly tasting without any bitterness of drug as confirmed by the taste panel.抄録全体を表示PDF形式でダウンロード (887K) -
Hideyuki Goto, Yoshiyasu Terao, Shuji Akai原稿種別: Regular Article
2009 年 57 巻 4 号 p. 346-360
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーForty-eight kinds of isoflavones (8), thirty-one isoflavanes (9), and forty-seven biphenyl-ketones (10, 10′) were synthesized from eleven kinds of substituted phenols (11) and six phenylacetic acids (12). Among them, seventy-five compounds are new. The radical scavenging activities of these compounds were evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) at pH 6.0. We found that thirty-nine out of forty-three compounds having a catechol moiety on either the A- or the B-ring exhibited a high activity (ED50=12—54 μM) similar to that of catechin. In these cases, the remaining part of their structure seemed to have little effect on their activity. Many 6- or 8-hydroxyisoflavanes (9E—I) and their biphenyl-ketone derivatives (10E—H) also showed a high activity (ED50=<50 μM), while all of their corresponding isoflavones (8E—I) were not active at all. The 7-hydroxyisoflavanes having either an additional hydroxyl group at the C5-position (9D) or a methoxy group at the C6-position (9J) presented a high activity (ED50=26—32 μM). This study suggests that natural isoflavones have the possibilities of exhibiting antioxidant activities through the hydroxylation at the C6-, C8-, or C3′-position or the formation of the isoflavanes (9) and/or the biphenyl-ketone derivatives (10′) by metabolism or biotransformation.抄録全体を表示PDF形式でダウンロード (445K) -
Toshio Morikawa, Li-Bo Wang, Seikou Nakamura, Kiyofumi Ninomiya, Eri Y ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 361-367
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe methanolic extract from the flowers of Helichrysum arenarium L. MOENCH was found to show inhibitory effect on tumor necrosis factor-α (TNF-α, 1 ng/ml)-induced cytotoxicity in L929 cells. From the methanolic extract, 50 constituents including four new flavanone and chalcone glycosides named arenariumosides I (1), II (2), III (3), and IV (4) were isolated. The stereostructures of 1—4 were elucidated on the basis of chemical and physicochemical evidence. Among the constituents, naringenin 7-O-β-D-glucopyranoside (7), apigenin 7-O-β-D-glucopyranoside (14), apigenin 7-O-gentiobioside (16), and apigenin 7,4′-di-O-β-D-glucopyranoside (17) significantly inhibited TNF-α-induced cytotoxicity in L929 cells at 30 μM.抄録全体を表示PDF形式でダウンロード (244K) -
Surachai Nimgirawath, Phansuang Udomputtimekakul, Thongchai Taechowisa ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 368-376
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーA convenient and economical synthesis of 4-hydroxy-2,3-dimethoxybenzaldehyde has been developed. This was used as the starting material for the first total syntheses of (±)-isopiline, (±)-preocoteine, (±)-oureguattidine and (±)-3-methoxynordomesticine in which the key step involved formation of ring C of the aporphines by a radical-initiated cyclisation. Although (±)-3-methoxynordomesticine possesses weak antimicrobial activity, it inhibits the production of nitric oxide (NO), prostaglandin (PG)E2, tumor necrosis factor (TNF)-α, interleukin (IL)-1β and IL-6 and the expression of inducible nitric oxide synthase (iNOS) and cycloxygenase (COX)-2 in macrophages stimulated with LPS in vitro.抄録全体を表示PDF形式でダウンロード (341K) -
Taichi Ohshiro, Daisuke Matsuda, Kenichiro Nagai, Takayuki Doi, Toshia ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 377-381
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe selectivity of synthetic beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA : cholesterol acyltrasferase (ACAT), ACAT1 and ACAT2, was studied in cell-based assays using ACAT1- or ACAT2-expressing Chinese hamster ovary (CHO) cells. NBV274, 285 and 300 showed ACAT1 selective inhibition similar to that of natural beauveriolides I and III, NBV345 inhibited both isozymes with similar potency, but NBV281, 331 and 249 were found to selectively inhibit the ACAT2 isozyme. The structure–activity relationships indicated that a subtle structural difference in beauveriolide derivatives can affect the selectivity of inhibition of the ACAT isozymes.抄録全体を表示PDF形式でダウンロード (227K) -
Emi Tokuyama, Chiharu Matsunaga, Koichi Yoshida, Jean-Christophe Mifsu ...原稿種別: Regular Article
2009 年 57 巻 4 号 p. 382-387
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe purpose of the present study was to compare the palatability of the original and eight generic versions of famotidine orally disintegrating tablets by means of human gustatory sensation tests, a comparison of the release profiles, and using an automated taste sensor, the α-Astree Electronic Tongue. In the gustatory sensation test, the original product (Gaster®D, 10 mg) showed the lowest bitterness intensity. Among the eight generic products tested, the variance in the sweetness intensity was not great, but there were large variances in the intensity of bitterness, some of the generic products being significantly more bitter than that of the original product. On the other hand, some generic products show similar bitterness level as the original product. In a study of release profiles, the original product had the lowest release rates of both famotidine and aspartame; in comparison, some of the generic products had high release rates of famotidine and aspartame, even in the initial stages. Whereas some generic products had low release rates of famotidine and aspartame. Finally, sample solutions were analysed using the taste sensor. There was a good correlation between the taste predicted by principal component analysis and the Euclidean distance obtained by the taste sensor, and bitterness intensities obtained in the human gustatory tests.抄録全体を表示PDF形式でダウンロード (268K)
Notes
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Hitendra Shaligram Mahajan, Surendra Ganeshlal Gattani原稿種別: Notes
2009 年 57 巻 4 号 p. 388-392
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe purpose of this study was to develop nasal microparticles of metoclopromide employing gellan gum as a polymer by spray drying method. This method of microencapsulation is particularly less dependent on the solubility characteristics of the drug and polymer and is simple, reproducible, and easy to scale up. The microparticles were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, mucoadhesion, thermal analysis, X-ray diffraction (XRD) study and in vitro drug release. The microparticles so prepared had irregular shape and smooth but distorted surface morphology. They were negatively charged. The particle size ranged from 9.38 to 10.67 μm. Differential scanning calorimetry (DSC) studies revealed that metoclopromide was molecularly dispersed inside the microparticles. The swelling was increased with increase in amount of polymer. The release of drug from microparticles was moderately sustained without lag time and attributed to formation of hydrogel; ionically cross linked hydrogel was hypothesized. The formulation was found to be non toxic to nasal tissue. These in vitro preliminary results show that spray dried microparticles based on gellan gum could be suitable nasal delivery system for the administration of metoclopromide.抄録全体を表示PDF形式でダウンロード (1190K) -
Hidenori Kimura, Kohei Torikai, Ikuo Ueda原稿種別: Notes
2009 年 57 巻 4 号 p. 393-396
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe reagent-free C2–C7 thermal cyclization of a nonconjugated aryl–yne–carbodiimide yielded a dibenzo[b,g][1,8]naphthyridine derivative, whose congeners are known to possess fascinating pharmacological properties. This is the first heteroaromatic compound prepared by the thermal cycloaromatization of “nonconjugated” aryl–ynes.抄録全体を表示PDF形式でダウンロード (140K) -
Dae Sik Jang, Ga Young Lee, Yun Mi Lee, Young Sook Kim, Hang Sun, Dong ...原稿種別: Notes
2009 年 57 巻 4 号 p. 397-400
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーTwo new flavan-3-ols, 6-(2-pyrrolidinone-5-yl)-(−)-epicatechin (1) and 8-(2-pyrrolidinone-5-yl)-(−)-epicatechin (2), as well as five known compounds, (−)-epicatechin (3), (+)-catechin (4), proanthocyanidin B-4 (5), (+)-pinoresinol, and p-hydroxybenzoic acid, were isolated from an EtOAc-soluble extract of the roots of Actinidia arguta. The structures of compounds 1 and 2 were elucidated by spectroscopic data interpretation, particularly by extensive 1D- and 2D-NMR studies. All the isolates were evaluated in vitro for inhibitory activity on the formation of advanced glycation end products (AGEs). Of these, compounds 1—5 exhibited significant inhibitory activity against AGEs formation with IC50 values ranging from 10.1 to 125.2 μM.抄録全体を表示PDF形式でダウンロード (105K) -
Yong-Hui Li, Yi-Fang Yang, Kun Li, Li-Li Jin, Nian-Yun Yang, De-Yun Ko ...原稿種別: Notes
2009 年 57 巻 4 号 p. 401-404
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーIn the screening of biologically active constituents from Brassica rapa pollen, the supercritical CO2 fluid extract (SFE-CO2) showed potent 5α-reductase and aromatase inhibiting activity. The SFE-CO2 extract was separated by various chromatographic methods to give two new phytosterol derivatives, 24-methylenecholesterol linolenate (1) and cycloeucalenol linolenate (2), as well as eight known compounds, 24-methylenecholesterol palmitate (3), cycloeucalenol (4), pollinastanol (5), 24-methylenecholesterol (6), linolenic acid (7), palmitic acid (8), monolinolein (9) and monopalmitin (10), compounds 7 and 9 showed potent 5α-reductase inhibitory activity; compounds 1—6 and 10 showed potent aromatase inhibitory activity.抄録全体を表示PDF形式でダウンロード (118K) -
Hai-Tao Liu, Li-Jia Xu, Yong Peng, Xiu-Wei Yang, Pei-Gen Xiao原稿種別: Notes
2009 年 57 巻 4 号 p. 405-407
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーTwo new lignans, henricines A (1) and B (2), were isolated along with the eight known lignans, ganshisandrine (3), wulignan A2 (4), epiwulignan A1 (5), deoxyschisandrin (6), wulignan A1 (7), epischisandrone (8), schisantherin A (9), and schisandrol A (10), from the stems of Schisandra henryi. The structures of the new compounds were elucidated based on the spectral analysis, including 1D and 2D NMR experiments.抄録全体を表示PDF形式でダウンロード (136K) -
Yan Ren, Li Shen, De-Wu Zhang, Sheng-Jun Dai原稿種別: Notes
2009 年 57 巻 4 号 p. 408-410
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーTwo new sesquiterpenoids, lyratol C (1) and lyratol D (2), together with two known sesquiterpenoids, dehydrovomifoliol (3) and blumenol A (4), were isolated from the whole plant of Solanum lyratum. Their structures were established by spectroscopic analyses. In vitro, the four compounds showed significant cytotoxic activities against three human cancer cell lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and gave IC50 values in the range 3.7—8.1 μM.抄録全体を表示PDF形式でダウンロード (126K) -
Hisashi Matsuda, Junji Akaki, Seikou Nakamura, Yoshie Okazaki, Hiroaki ...原稿種別: Notes
2009 年 57 巻 4 号 p. 411-414
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThe methanolic extract and its ethyl acetate-soluble fraction from the dried powder of cultured Cordyceps sinensis mycelium showed cytotoxic effects on promyelocytic leukemia HL-60 cells. Sitosterol (1), 5α,8α-epidioxy-22E-ergosta-6,22-dien-3β-ol (2), 5α,8α-epidioxy-22E-ergosta-6,9(11),22-trien-3β-ol (3), 5α,6α-epoxy-5α-ergosta-7,22-dien-3β-ol (4), and ergosterol (5) were isolated from the ethyl acetate fraction. Among the isolated compounds, 2—4 with a peroxide ring or an epoxide ring showed substantial cytotoxic activity with IC50 values of 7.3—7.8 μg/ml, but 1 and 5 showed only moderate activity. Furthermore, apoptosis of HL-60 cells was observed 24 h after treatment with 2—4 (10, 20 μg/ml) using the TdT-mediated dUTP nick-end labeling method, and their apoptosis-inducing activities are suggested to be dependent on the activation of caspases-3/7. To the best of our knowledge, this is the first report of the isolation of sterol constituents (1—5) from cultured C. sinensis mycelium.抄録全体を表示PDF形式でダウンロード (158K) -
Rehan Khan, Abdul Malik, Achyut Adhikari, Mohammad Irfan Qadir, Muhamm ...原稿種別: Notes
2009 年 57 巻 4 号 p. 415-417
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーConferols A (1) and B (2), the new 4-hydroxyisoflavones, have been isolated from the dichloromethane sub-fraction of the methanolic extract of Caragana conferta along with 3′,5′-dihydroxy, 7,4′-dimethoxyisoflavone (3), E-cinnamic acid (4), tetracosyl 3,4-dihydroxy-E-cinnamate (5), docosyl 3,4-dihydroxy-E-cinnamate (6), β-sitosterol (7), β-sitostrerol 3-O-β-D-glucopyranoside (8), stigmasterol (9) and lupeol (10), respectively, reported for the first time from this species. The structures of the new compounds were elucidated through spectroscopic techniques including MS and 2D-NMR. The compounds 1—3 showed significant anti-inflammatory activity in the respiratory burst assay.抄録全体を表示PDF形式でダウンロード (85K) -
Xiao-ru Hu, Jun-shan Yang, Xu-dong Xu原稿種別: Notes
2009 年 57 巻 4 号 p. 418-420
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーThree new sesquiterpene glycosides, 8β,9β-epoxy-4α-hydroxy-5αH-lindan-7(11)-en-8α,12-olide-15-O-β-D-glucopyranoside (1, sarcaglaboside F), 4α-hydroxy-5α,8βH-lindan-7(11)-en-8α,12-olide-15-O-β-D-glucopyranoside (2, sarcaglaboside G), 4α-hydroxy-5α,8βH-eudesman-7(11)-en-8α,12-olide-15-O-β-D-glucopyranoside (3, sarcaglaboside H), together with five known compounds, chloranoside A (4), sarcaglaboside C (5), dihydrovomifoliol-O-β-D-glucopyranoside (6), 9-hydroxy-heterogorgiolide (7) and chloranthalactone B (8), were isolated from Sarcandra glabra THUMB. NAKAI. The structures and relative configurations of three new compounds were determined on the basis of their spectroscopic data and chemical evidence.抄録全体を表示PDF形式でダウンロード (125K) -
Hajime Maeda, Yosuke Matsuo, Takashi Tanaka, Isao Kouno原稿種別: Notes
2009 年 57 巻 4 号 p. 421-423
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーA new ellagitannin dimer named euscaphinin was isolated from the leaves of Euscaphis japonica (THUNB.) KANITZ. The structure of this dimer was determined on the basis of spectroscopic and chemical evidence. The resulting structure indicated that it was produced by intermolecular C–O oxidative coupling between the galloyl groups of molecules of 1(β)-O-galloyl pedunculagin, the major ellagitannin of the leaves. The ellagitannins were not detected in the bark and wood part of the plant. This is the first example of the isolation of ellagitannins from Staphyleaceaeous plants.抄録全体を表示PDF形式でダウンロード (133K) -
Qing-Song Ye, Ming-Jin Xie, Wei-Ping Liu, Xi-Zhu Chen, Yao Yu, Qiao-We ...原稿種別: Notes
2009 年 57 巻 4 号 p. 424-427
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーDiiodo-, dibromo- and dichloro-platinum(II) complexes containing L-histidine ligand were prepared. Their spectra and X-ray crystal structure of the dibromo-platinum(II) complex were described. Only the dichloro-platinum(II) complex showed comparable cytotoxic activity with carboplatin against A549/ATCC, HT-29, and LNcap cell lines. Nevertheless the complexes with COOH-substituted ligands histidine may be good starting materials to synthesize targeting platinum complexes since they could be easily linked to suitable carrier molecules via esterification.抄録全体を表示PDF形式でダウンロード (230K) -
Ratchanaporn Chokchaisiri, Channarong Suaisom, Siriluk Sriphota, Anon ...原稿種別: Notes
2009 年 57 巻 4 号 p. 428-432
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーOne new dihydrochalcone, dihydromonospermoside (7), was isolated from the flowers of Butea monosperma together with three known chalcones, butein (2), monospermoside (4) and isoliquiritigenin (8), one flavone, 7,3′,4′-trihydroxyflavone (6), four flavanones, (−)-butin (1a), (−)-butrin (3a), (+)-isomonospermoside (5b) and (−)-liquiritigenin (9a), and three isoflavones, formononetin (10), afrormosin (11) and formononetin-7-O-β-D-glucopyranoside (12). The structure of the new compound was elucidated by spectroscopic techniques whereas those of the known compounds were identified by comparisons of spectroscopic and some physical data with those of reported compounds. The absolute configurations at the 2-position of the flavanones 1a, 3a, 5b and 9a were established to be 2S, 2S, 2R and 2S, respectively, by circular dichroism spectral measurements and were confirmed by comparison of the optical rotations with those of reported values and by enzymic hydrolysis of the glucosides to the corresponding aglycones. The isolated flavonoids exhibited varying antimycobacterial activity with the chalcone 2 being the most active compound (MIC 12.5 μg/ml).抄録全体を表示PDF形式でダウンロード (151K) -
Di Xu, Yu Sheng, Zhong-Yu Zhou, Rong Liu, Ying Leng, Ji-Kai Liu原稿種別: Notes
2009 年 57 巻 4 号 p. 433-435
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーA new drimane sesquiterpenoid, 3-keto-drimenol (1), were isolated from cultures of the basidiomycete Clitocybe conglobata together with 3β-hydroxy-11-acetyldrimene (2), 3β-hydroxydrimenol (3), 11,12-dihydroxydrimene (4), 3β-hydroxy-11,12-O-isopropyldrimene (5), and 3β,11,12-trihydroxydrimene (6). Their structures were established from MS and NMR experiments. Compounds 1, 3, and 6 showed inhibitory activities against two isozymes of 11β-hydroxysteroid dehydrogenases with IC50 1.7—8.0 μg/ml (human 11β-HSD1), 10.7—24.1 μg/ml (mouse 11β-HSD1); 177.0—220.0 μg/ml (human 11β-HSD2), 250.5—500.2 μg/ml (mouse 11β-HSD2), respectively, which catalyze the interconversion of active cortisol and inactive cortisone.抄録全体を表示PDF形式でダウンロード (87K)
Communicatins to the Editor
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Weiwei Qin, Naoki Kakusawa, Yichen Wu, Shuji Yasuike, Jyoji Kurita原稿種別: Communications to the Editor
2009 年 57 巻 4 号 p. 436-438
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーSimple and mild Cu-mediated arylation of various amines by use of tetraarylantimony acetate (Ar4SbOAc) is described. The Ullmann-type condensation of Ar4SbOAc with aliphatic and electron rich aromatic amines proceeded efficiently in the presence of copper(II) acetate. The arylation can be carried out under aerobic conditions without care of exogenous oxygen. This simple procedure exceeds the conventional Ullmann condensation which often requires harsh reaction conditions.抄録全体を表示PDF形式でダウンロード (169K) -
Nahoko Uchiyama, Ruri Kikura-Hanajiri, Nobuo Kawahara, Yuji Haishima, ...原稿種別: Communications to the Editor
2009 年 57 巻 4 号 p. 439-441
発行日: 2009/04/01
公開日: 2009/04/01
ジャーナル フリーA new type of designer drug, a cannabinoid analog (1), was found in a herbal product distributed on the illegal drug market in Japan in expectation of its narcotic effect. The structure of 1 was identified by LC-MS, GC-MS, high-resolution MS, and NMR analyses. Compound 1 showed a molecular weight of 332, and accurate mass measurement exhibited its elemental composition to be C22H36O2. Together, the mass and NMR spectrometric data revealed that 1 was (1RS,3SR)-3-[4-(1,1-dimethyloctyl)-2-hydroxyphenyl]cyclohexan-1-ol, which was first synthesized in 1979 by a group at Pfizer Inc. and reported as a potent cannabinoid analog possessing cannabinoid receptor binding activity and analgesic activity in the 1990s. This is the first report to identify a cannabinoid analog in an illegal drug.抄録全体を表示PDF形式でダウンロード (95K)
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