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Volume 14, Issue 4
Displaying 1-18 of 18 articles from this issue
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Masatomo Hamana, Tsuyoshi Nagayoshi1966 Volume 14 Issue 4 Pages 319-323
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNitrations of 6-chloro-, 6-bromo-, 6-methyl-, 6-methoxy-quinoline and quinoline 1-oxides with potassium nitrate in sulfuric acid were re-examined by varying the concentration of the acid and the reaction temperatures. The orientation of reaction was found to be more markedly dependent upon the concentration of sulfuric acid rather than the reaction temperature ; generally, the activity of the 4-position toward nitration became most remarkable by use of 75∼85% sulfuric acid.View full abstractDownload PDF (612K) -
Shunsaku Shiotani, Kemmotsu Mitsuhashi1966 Volume 14 Issue 4 Pages 324-329
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to test the pharmacological activities, some derivatives of 1, 2, 3, 4, 5, 6-hexahydro-1, 5-methanobenzo [e] [1, 3] diazocine were synthesized.cis-1, 2, 3, 4-tetrahydro-1, 3-naphthalenediamine (V) was prepared by Schmidt reaction of cis-4-amino-1, 2, 3, 4-tetrahydro-2-naphthoic acid (IV) which was obtained by catalytic reduction of methyl 4-hydroximino-1, 2, 3, 4-tetrahydro-2-naphthoate (I), followed by cyclization and hydrolysis. Reduction of N, N′-diacetyl-(VIa) and N, N′-diformyl-(VIb) derivatives of V with lithium aluminum hydride afforded N, N′-diethyl-(VIIa) and N, N′-dimethyl-(VIIb) derivatives, respectively. Condensation of VIIa with formaldehyde and benzaldehyde gave 2, 4-diethyl-(VIIIa) and 2, 4-dimethyl-3-phenyl-1, 2, 3, 4, 5, 6-hexahydro-1, 5-methanobenzo [e] [1, 3]-diazocine (VIIIc). Similarly, 2, 4-dimethyl derivatives (VIIIb) and (VIIId) were prepared.View full abstractDownload PDF (737K) -
Hisashi Nogami, Tsuneji Nagai, Akira Suzuki1966 Volume 14 Issue 4 Pages 329-338
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe disk of sulfonamide was made by compression of the powder and the dissolution rate was measured by rotating it in water under various conditions. The results obtained are : 1. The concentration-time curve of dissolution was obtained with a good reproducibility and it did not depend on the thickness of disk, the size and shape of the flask which contained the liquid, and the depth of the disk from water level. 2. The dissolution rate constant, KT, did not depend on the surface area of the disk and the volume of the liquid of 50 to 200 ml. During the dissolution experiment, disintegration of disk could not be considered to occur. 3. KT did not depend on the compressional pressure to make disk under 1 to 5 tons/cm2. This showed that the dissolution depended on the apparent geometrical surface area, not on the intrinsic surface area of solid. 4. KT was proportional to the square root of rotating velocity of the disk. 5. The activation energy of dissolution of sulfadiazine was about 3.5 Kcal./mole. 6. The values of KT of five kinds of sulfaonamides were quite coincident with the values calculated according to the Arnold equation. The values of saturated concentration, CO, were coincident with the values of solubility, CS, observed. 7. From the results obtained, it would be possible to give the following conclusions : I) From the measurement of dissolution rate by the rotating disk method, KT and CO can be obtained separately with a high confidence on the value. ii) The dissolution of sulfonamide is in accordance with the Noyes-Nernst equation concerning the transport controlled dissolution. The Levich Equation is also established.View full abstractDownload PDF (995K) -
Hisashi Nogami, Tsuneji Nagai, Akira Suzuki1966 Volume 14 Issue 4 Pages 339-350
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe following results were obtained on the dissolution of sulfadiazine in various aqueous solution. 1. On the dissolution in sucrose solution, with an increase of sucrose concentration, the saturated concentration, CO was increased a little, and the dissolution constant, KT, was decreased with an increase of viscosity following an increase of the concentration. The dissolution rate by practical representation, KT×CO, became smaller with an increase of sucrose concentration. The dissolution was in accordance with the Noyes-Nernst model, and CO was coincident with the solubility, CS.2. On the dissolution in sodium chloride solution, both KT and CO were decreased with an increase of the concentration of sodium chloride. The dissolution was in accordance with the Noyes-Nernst model.3. On the dissolution in sodium hydroxide solution, both KT and CO were increased with an increase of the concentration of sodium hydroxide. The dissolution was in accordance with the Nernst-Brunner model. The increase of KT was considered to be due to the increase of diffusion coefficient of sodium hydroxide in the presence of sodium salt of sulfadiazine. 4. The dissolution in Na2HPO4 solution, in Mc'Ilvaine buffer solution and in hydrochloric acid solution were in accordance with the Higuchi model, and as an increase of concentration of the solution, CO was increased by the change of hydrogen ion concentration. 5. The dissolution in urea solution did not fit to any of the model in Table I.View full abstractDownload PDF (1063K) -
Hisashi Nogami, Tsuneji Nagai, Koji Ito1966 Volume 14 Issue 4 Pages 351-357
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dissolution rates of benzoic acid derivatives in water and in urea solution were measured by rotating disk method. The data of the dissolution in urea solution showed a good agreement qualitatively with the process in which there exist some reaction and the equilibrium is reached rather slowly in the diffusion layer and the solutes are transferred into the bulk solution under non-equilibrium state. That is, the dissolution rate constant, KT, and the saturated concentration, CO, showed the dependence on the lapse of time, and the initial dissolution rate constant, KT(t→o), was almost the same as the value of KT observed on the dissolution in water.View full abstractDownload PDF (676K) -
Mamoru Kamiya, Tatsunori Hamaoka, Takao Kwan1966 Volume 14 Issue 4 Pages 358-362
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe ratio of the reaction rates of the photo-excited quinones with isopropyl alcohol as compared with their deactivation has been determined using methylnaphthoquinone, naphthoquinone, anthraquinone and dichloronaphthoquinone as photocatalysts. The sequence of the ratios was found to be methylnaphthoquinone>naphthoquinone>anthraquinone>dichloronaphthoquinone. Attempts were made to correlate this sequence with the electronic energies of the photo-excited state of the respective quinone as well as of the corresponding semiquinone radical. The importance of the life-time of the photo-excited methylnaphthoquinone was pointed out in connection with its highest photocatalytic activity.View full abstractDownload PDF (541K) -
Keiichi Nitta, Yuzuru Yamamoto, Toshimi Inoue, Toshiko Hyodo1966 Volume 14 Issue 4 Pages 363-369
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBiogenesis of oospolactone (I) and oosponol (II) from a fungus, Oospora astringenes were studied by using glucose-[1-14C], glucose-[6-14C], malonate-[2-14C], formate-[14C], and uniformly labelled glucose-[14C]. Degradation methods of the two metabolites were established and the progress of cultivation was also studied. The isotope experiments suggest that the skeletons of the two metabolites are synthesized from five C2-units according to the ''acetate-malonate condensation'' and one C1-unit. C1unit is incorporated as methyl-C (carbon 11) in I, on the other hand, as =CH- (carbon 9) which participates to form the lactone ring in II. It is interesting that these two isocoumarins from the same culture have the different origin of lactone ring.View full abstractDownload PDF (787K) -
Tetsuji Kametani, Osamu Umezawa1966 Volume 14 Issue 4 Pages 369-375
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the previous papers the reactions between aromatic, aliphatic and heterocyclic carboxylic acid hydrazides and either chloral or bromal in various alcohols were attempted and respective esters were obtained. In this paper the reactions of aromatic and aliphatic acid hydrazide with chloral in the presence of various amines were examined, leading eventually to reveal the formation of our expected acid amides as are shown in Table I and II. The intermediates in this reaction, 1-benzoyl-2-(2, 2, 2-trichloroethylidene) hydrazine (III : R=C6H5-, X=Cl) was found to form the amides (VI) when heated in amines. This fact indicated that the acid hydrazides converted to their amides through III.View full abstractDownload PDF (835K) -
Shiro Takahashi, Hideo Kano1966 Volume 14 Issue 4 Pages 375-385
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of 1-methyl- or 1, 2-dimethyl-3-methoxybenzimidazolium iodide (I or II) with various nucleophilic reagents (CN-, OH-, RO-, amines etc.) have been investigated. Most of these reagents reagents react with I to give the corresponding 2-substituted 1-methylbenzimidazole.The reaction of II with these reagents generally affords 1, 2-dimethylbenzimidazole (V) losing its methoxy group. Only with potassium cyanide, II undergoes substitution concurrently to give a mixture of 1, 2-dimethyl-6-benzimidazolecarbonitrile and V. The reaction mechanisms have been discussed as compared with those of Nalkoxypyridinium salt, and a possible zwitterion intermediate for the reaction of I is noted.View full abstractDownload PDF (1108K) -
Hisao Matsumoto, Hisakichi Matsumura, Sadao Iguchi1966 Volume 14 Issue 4 Pages 385-391
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA method of determining the small quantities of nonionic surfactants (Tween and Brij types) in the presence of polyethyene glycol was devised utilizing the increase of solubility of yellow AB. With this method, permeation of nonionic surfactants through cellulose membrane was investigated and compared with the results obtained with phosphomolybdic acid method. As the results, it became evident that impurities, especially low molecular weight polyethylene glycol, permeate rapidly, but permeation of nonionic surfactant molecules is negligible. To obtain the magnitude of interaction between benzocaine or sodium salicylate and Tween 80, equilibrium dialysis experiments were successfully carried out employing the cellulose membrane.View full abstractDownload PDF (790K) -
Hisao Matsumoto, Hisakichi Matsumura, Sadao Iguchi1966 Volume 14 Issue 4 Pages 391-398
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo kinds of dialysis apparatus were constructed and deviced to permit rapid dialysis of drug molecules. Applicability of theoretical equations of dialysis was tested and proved to be well applicable even if any stirring was not supplied. But it was found that results of dialysis must be compared and discussed among the same condition of dialysis. Dialysis from saturated solutions of benzocaine in Tween 80 solutions was studied and it was concluded that drug molecules in the micellar phase are transferred to the aqueous phase rapidly corresponding to decrease of the concentration of the drug in the aqueous phase even if any stirring is not supplied, then they participate in the dialysis to the outer fluid.View full abstractDownload PDF (771K) -
Hisao Matsumoto1966 Volume 14 Issue 4 Pages 398-406
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to investigate the rapidity of transfer of drug molecules from micellar to aqueous phase in nonionic surfactant solutions, theoretical equations were derived assuming that the transfer occurs instantaneously corresponding to the decrease of drug concentration in the aqueous phase. Applicability to the equations was examined with static dialysis of methylparaben, propylparaben and benzocaine in Tween 80 solutions using two kinds of dialysis apparatus at 30°. It was proved that these results were well applicable to the equations and the transfer is instantaneous. But a little increase of dialysis beyond the theoretical value was observed when drug molecules were partitioned predominantly into the micellar phase and the ratio, γ, became large. This phenomenon was attributed to direct dialysis from the micellar phase. Therefore the direct dialysis could be neglected when the ratio, γ, was relatively small. When volume of the outer fluid was enough large, decrease of drug concentration in the inner surfactant solution also became theoretically the first order process and its apparent decreas■g coefficient, Pd, became P′/γ. These relationships were well applied to the dialysis of various drugs.View full abstractDownload PDF (750K) -
Akira Takamizawa, Yoshiro Sato, Sachiko Tanaka, Hisako Itoh1966 Volume 14 Issue 4 Pages 407-413
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was shown that a new thiamine derivative which was obtained from the reaction of the neutral form of thiamine (I) with diethyl benzoylphosphonate (II) should be formulated as 2-phenyl-3-oxo-4-(2-methyl-4-amino-5-pyrimidyl) methyl-5-methyl-6-(2-benzoyloxy) ethyl-2, 3-dihydro-4H-1, 4-thiazine (IV). A novel benzoylation reaction accompanied by the rearrangement from thiazole to 1, 4-thiazine is also described.View full abstractDownload PDF (750K) -
Nobuo Tanaka, Goichi Hirata, Isamu Utsumi1966 Volume 14 Issue 4 Pages 414-419
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhase separation of PAA by various cationic drugs has been investigated as a function of temperature, polymer and added drug concentration. There exists a temperature Tp at which the PAA-drug aqueous solution separates into two phases (liquid-liquid or solid-liquid). The Tp changes remarkably not only with PAA or added drug concentration, but also with the basic structure of drug molecules or valences of drug cations. The decreasing order of the Tp is O-benzoylthiamine>thiamine>N-methylephedrine>ephedrine>piperidine>N, N-dimethylaniline>N-methylaniline≒aniline>pyridoxine≒pyridine.View full abstractDownload PDF (638K) -
Yutaka Morita1966 Volume 14 Issue 4 Pages 419-426
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNMR spectra of phenazine derivatives were completely analyzed by the theoretical treatment of observed signals. These assignments have shown the proton signals of phenazine as A2B2 type. Various J values have been testified by the examination of the spectra of substituted derivatives. These analyses are expected to be effective tools for structural elucidation of synthetic unknown substituted phenazine derivatives arising from the ambiguity of their synthetic routes.View full abstractDownload PDF (736K) -
Yutaka Morita1966 Volume 14 Issue 4 Pages 426-432
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMass spectra of phenazine, phenazine mono-N-oxide, phenazine di-N-oxide, 1-methyl-, 1-methoxy-, 2-methoxy phenazines were analyzed. The results disclosed that their fragmentation pathways were comparable with the aromatic tricyclic compounds. And chromatographic behaviors of phenazine derivatives were examined using mainly 20 kinds of chlorophenazines considering the polarisabilities of phenazine nuclei.View full abstractDownload PDF (603K) -
Yutaka Morita1966 Volume 14 Issue 4 Pages 433-435
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe NMR spectra of chlorophenazines were measured and analyzed as the one of representative examples of substituted phenazines. Comparing with previously reported methoxyphenazines, ring protons of chlorophenazines showed weakly influenced signal patterns in which the anisotropic effects of chlorine atoms were observed in opposite sign to the methoxyl's. The significant abnormality in its shielding power of beta substituent on phenazine ring is conceivable to propose an additional interest for clarification of the reactivity and the polarizability of beta substituent. Concerning to the reactivity of substituent, methyl and methoxyl proton shifts of alpha and beta substituted phenazines were examined giving explicit descrimination in their absorption region as were seen in ring protons.View full abstractDownload PDF (423K) -
Shigenobu Okuda, Yuya Nakayama, Kyosuke Tsuda1966 Volume 14 Issue 4 Pages 436-441
Published: April 25, 1966
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo new antibiotics, 7-desacetoxyhelvolic acid and helvolinic acid were isolated from the culture broth of Cephalosporium caerulens. Characterization and structural studies of these substances are described.View full abstractDownload PDF (565K)
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