YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
1,5-Benzothiazepine誘導体の合成(第4報)dl-cis-3-Acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one Hydrochlorideの光学分割
井上 博純竹尾 聰河津 光高釘田 博至
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1973 年 93 巻 6 号 p. 729-732

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Preparation of d-cis-3-acetoxy-5-[2-(dimethylamino)ethyl]-2, 3-dihydro-2-(p-methoxyphenyl)-1, 5-benzothiazepin-4(5H)-one hydrochloride (IIId) with potent coronary vasodilatory activity is described. Attempted resolution of III, IX, and VI with various optically active acids was unsuccessful. VIIId was barely obtained by numerous repeated recrystallization of d-10-camphorsulfonate of VIII in a low yield. On the other hand, resolution of V with cinchonidine was carried out successfully. VIl was also obtained by resolution of VI with ephedrine. IIId and IIIl were easily prepared from Vd and Vl, respectively.

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