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Process for preparation of lopinavir intermediate
专利权人:
LUPIN LTD
发明人:
MAHAJAN PRAVIN RAGUNATH,MAHAJAN PRAVIN RAGUNATH,SINGH GURVINDER PAL,SINGH GURVINDER PAL,RAY PURNA CHANDRA,RAY PURNA CHANDRA,KARNALKAR DABEER RAUF,KARNALKAR DABEER RAUF
申请号:
IN2745/MUM/2013
公开号:
IN2013MU02745A
申请日:
2013.08.22
申请国别(地区):
IN
年份:
2015
代理人:
摘要:
The present invention provides aprocess for the preparation of lopinavir intermediate (2S,3S,5S)-2-Amino-3-hydroxy-5-[2S-(l-tetrahydro-pyrimid-2- onyl)-3-methyl butanoyl]amino-l,6-diphenylhexane (S)-Pyroglutamic acid salt(II) comprising: (a) N-debenzylation of (2S,3S,5S)-2-N,N-dibenzylamino-3-hydroxy- 5-[2S-(l-tetrahydro-pyrimid-2-onyl)-3-methyl butanoyl]amino-1,6- diphenylhexane (III) to get (2S,3S,5S)-2-amino-3-hydroxy-5-[2S-(l-tetrahydro-pyrimid-2-onyl)-3-methyl butanoyI]amino-l,6-diphenylhexane (IV) in the presence of transition metal catalyst on activated carbonand formic acid salt in alcoholic solvent, (b) treatment of the reaction mixture with aqueous inorganic base and (c) reaction with L-pyroglutamic acid.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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