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STABLE R (+) -LANSOPRAZOLE AMINE SALT AND A PROCESS FOR PREPARING THE SAME
专利权人:
WATSON PHARMA PRIVATE LIMITED
发明人:
BHANU, MANJUNATH NARAYAN,NAIK, SAMIR,BODKHE, ARJUN
申请号:
NZ58915009
公开号:
NZ589150A
申请日:
2009.05.12
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
The disclosure relates to a solid R-(+)-Iansoprazole butylamine salt and a process for preparing a stable R-(+)-Iansoprazole butylamine salt, wherein the process comprises the steps of:optically resolving racemic lansoprazole, isolating R-(+)- lansoprazole, and reacting the isolated R-(+)-Iansoprazole with a butylamine to form a stable R-(+)lansoprazole butylamine salt; (a) treating racemic lansoprazole with R-(+)-2,2'-dihydroxy-I,I'- binaphthyl ("R-(+)BINOL") in a suitable solvent to form the inclusion complex of R-(+)lansoprazole with R-(+)-BINOL;(b) removing the inclusion complex of R-(+)-Iansoprazole with R-(+)- BINOL prepared in step (a) from the solvent and adding a mixture of organic solvents; (c) crystallizing the R-(+)-Iansoprazole - R-(+)-BINOL inclusion complex from the mixture of organic solvents; (d) enriching the R-(+)-Iansoprazole - R-(+)-BINOL inclusion complex to obtain a purity of more than about 97% e.e.; (f) cleaving the enriched R-(+)-Iansoprazole - R-(+)BINOL inclusion complex; (g) separating the R-BINOL and R-(+)-Iansoprazole; (h) isolating the R-(+)-Iansoprazole; and (i) reacting the R-(+)-Iansoprazole with a butylamine to form a stable R-(+)lansoprazole butylamine salt.
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