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
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概要
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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.
- 公益社団法人日本薬学会の論文
- 1973-06-25
著者
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井上 博純
Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd, .
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竹尾 聰
田辺製薬株式会社有機化学研究所
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釘田 博至
田辺製薬有機研究所
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井上 博純
田辺製薬株式会社有機化学研究所
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河津 光高
田辺製薬株式会社有機化学研究所
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釘田 博至
田辺製薬株式会社有機化学研究所
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釘田 博至
Organic Chemistry Research Laboratory:tanabe Seiyaku Co. Ltd.
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井上 博純
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd .
関連論文
- Enantioselective Reduction of meso-Cyclic-1,2-dicarboxylic Anhydrides and 1,2-Dicarboximides : Asymmetric Synthesis of Bicyclic Lactones and Hydroxylactams
- A New Enantioselective Synthesis of (2R, 3S)-3-(4-Methoxyphenyl)glycidic Ester via the Enzymatic Hydrolysis of erythro-N-Acetyl-β-(4-methoxyphenyl)serine
- A New Synthetic Route to 1,5-Benzothiazepines. Synthesis of Derivatives of Diltiazem
- Synthesis of the Metabolites of Clentiazem
- Asymmetric Reduction of Aromatic Ketones. II. An Enantioselective Synthesis of Methyl (2R, 3S)-3-(4-Methoxyphenyl)glycidate
- Synthesis of the Optically Active trans-Isomers of Diltiazem and Their Cardiovascular Effects and Ca-Antagonistic Activity
- Synthesis of N-Substituted C-Normorphinans and Their Pharmacological Properties
- Reactions of 3-Phenylglycidic Esters. V. Reaction of Methyl 3-(4-Methoxyphenyl) glycidate with 2-Nitroaniline and Synthesis of 1,5-Benzodiazepine Derivatives
- Reaction of 3-Phenylglycidic Esters. III. Reaction of cis-3-Arylglycidic Esters with Various Thiophenols
- Reaction of 3-Phenylglycidic Esters. IV. Reaction of Methyl 3-(4-Methoxyphenyl) glycidate with 2-Nitrophenol and Synthesis of 1,5-Benzoxazepine Derivatives