PRODUCTION OF PERHYDRO-1,4-THIAZEPINE DERIVATIVE

PURPOSE:To obtain the titled substance useful as a synthetic intermediate for hypotensor, in high yield and efficiency, by condensing a reactive derivative of a cysteine derivative at the carboxy group or its acid addition salt optionally in the presence of a base. CONSTITUTION:A reactive derivative...

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Bibliographic Details
Main Authors NAKAZAWA JUNICHI, MIYAOKA TAKEO
Format Patent
LanguageEnglish
Published 18.06.1988
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PURPOSE:To obtain the titled substance useful as a synthetic intermediate for hypotensor, in high yield and efficiency, by condensing a reactive derivative of a cysteine derivative at the carboxy group or its acid addition salt optionally in the presence of a base. CONSTITUTION:A reactive derivative of a compound of formula I (R is 2-thienyl or 3-thienyl) at the carboxyl group or its acid addition salt is subjected to condensation reaction optionally in the presence of a base to obtain the compound of formula II. The reaction is carried out at 30-120 deg.C for 1-10hr when the reactive derivative is lower alkyl ester. For performing cyclization reaction with an active ester, the reaction is carried out in a halogenated hydrocarbon solvent in the presence of a base (e.g. pyridine) at -50-50 deg.C for 1-10hr.
Bibliography:Application Number: JP19870137319