PRODUCTION OF OPTICALLY ACTIVE PIPERAZINE DERIVATIVE AND ITS PRODUCTION INTERMEDIATE

PROBLEM TO BE SOLVED: To obtain an optically active body of piperazine-2-carboxylic acid-N-t- butylamide which is an intermediate for synthesizing an HIV protease inhibitor in high yield and in high optical purity by improving a means of optical resolution. SOLUTION: This production of optically act...

Full description

Saved in:
Bibliographic Details
Main Authors SAKAI KENICHI, MURAKAMI NAOMICHI, TOBIYAMA TADASHI
Format Patent
LanguageEnglish
Published 18.02.1997
Edition6
Subjects
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online AccessGet full text

Cover

More Information
Summary:PROBLEM TO BE SOLVED: To obtain an optically active body of piperazine-2-carboxylic acid-N-t- butylamide which is an intermediate for synthesizing an HIV protease inhibitor in high yield and in high optical purity by improving a means of optical resolution. SOLUTION: This production of optically active piperazine derivative is to react (RS)-piperazine-2-carboxylic acid-N-t-butyl amide compound of formula I (* expresses the position of an asymmetric carbon atom) with an optically active N-acylated amino acid of formula II (R is a 1-6C alkyl, etc.; Ar us 1-3 of 1-6C alkyl, etc.) 10 a solvent and form a diastereomer salt of formula III, while separate the other diastereomer salt from the solvent selectively, decompose the separated diastereomer and obtain optically active piperazine-2- carboxylic acid-N-t-butylamide.
Bibliography:Application Number: JP19950200098