PRODUCTION OF 1,5-BENZOTHIAZEPINE DERIVATIVE

PROBLEM TO BE SOLVED: To obtain the subject compound in a short time in a high yield by intramolecular cyclization of a specific propionic acid derivative in the presence of an α-chlorocarboxylic acid. SOLUTION: This compound, a 1,5-benzothiazepine derivative (salt) of formula II, is obtained by int...

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Bibliographic Details
Main Authors BOESTEN WILHELMUS HUBERTUS JOS, PLAUM MARCUS JOSEPH MARIA
Format Patent
LanguageEnglish
Published 13.01.1998
Edition6
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PROBLEM TO BE SOLVED: To obtain the subject compound in a short time in a high yield by intramolecular cyclization of a specific propionic acid derivative in the presence of an α-chlorocarboxylic acid. SOLUTION: This compound, a 1,5-benzothiazepine derivative (salt) of formula II, is obtained by intramolecular cyclization of (A) a propionic acid derivative of formula I (R1 is H, an alkyl or alkoxy; R2 is H or a halogen; R3 is H or an alkyl) in a non-halogenated solvent in the presence of (B) an α- chlorocarboxylic acid as carboxylic acid z (pref. trichloroacetic acid). It is preferable that the amount of the compound B to be used is 0.1-100mol% based on the amount of the component A. The derivative obtained by this method is alkylated and/or acrylated to obtain diltiazem.
Bibliography:Application Number: JP19970062592