OPTICALLY ACTIVE 1,5-BENZOTHIAZEPINE DERIVATIVE

Title:

OPTICALLY ACTIVE 1,5-BENZOTHIAZEPINE DERIVATIVE

Document Type and Number:

Japanese Patent JPS5519249

Kind Code:

A

Abstract:

NEW MATERIAL:A cis-form optically active 1,5-benzothiazepine dervative of the formula and its salts.

EXAMPLE: cis-(-)-2,3-Dihydro-3-[(4-methylpiperadinyl) methyl]-2-phenyl-1,5- benzothiazepin-4(5H)-one.

USE: Anti-acetylcholine and antitumor agents, having a greater action than the racemic isomer, and with weak side effects and low toxicity.

PROCESS: cis (±)-2,3-Dihydro-3-[(4-methylpiperadinyl) methyl]-2-phenyl-1,5- benzothiazepin-4(5H)-one is reacted with an optically active acid, e.g. (+) or (-)- tartaric acid in a solvent, e.g. CH3OH, to dissolve the (+) and (-) optically active salts which deposit due to the solubility difference in water. The solution is neutralized with Na2CO3, etc. to give the compound of the formula.

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Inventors:

IZUMI KIHACHIROU
HORI MIKIO
OONO SACHIO
MIZUKOSHI SEISHI
KATOU KAZUO
YAMAMOTO HAJIME
NAGASAKA MITSUAKI
NAKAMURA YOSHIKI
MORI MAKOTO

Application Number:

JP9299878A

Publication Date:

February 09, 1980

Filing Date:

July 29, 1978

Export Citation:

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Assignee:

MARUKO PHARMACEUTICAL CO

International Classes:

C07D281/10; A61K31/55; A61K31/554; A61P1/04; (IPC1-7): A61K31/55; C07D281/10

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Next Patent: CEPHALOSPORIN ANALOG, OR ITS SALTS, THEIR PREPARATION, AND PREVENTIVE AND REMEDY FOR MICROBISM