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DIHYDROETORPHINES AND THEIR PREPARATION
专利权人:
EURO-CELTIQUE S.A.
发明人:
WHITELOCK, STEVE,HARDING, DEBORAH PHYLLIS,TURNER, CARL DAVID
申请号:
NZ59310209
公开号:
NZ593102A
申请日:
2009.12.04
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Abstract - 593102 Disclosed is a process for the preparation of a compound of formula (VI) such as S-dihydroetorphine, or a salt thereof, wherein: R1 and R2 are independently C1-8straight-chained alkyl and * represents a (S) stereocentre) comprising reacting a compound of formula (IV) with a compound of formula R2M(X)p, wherein R2 is C1-8 straight-chained alkyl, M is a metal, X is halide and p is 1 or 0 (and preferably where R2M(X)p is MeMgBr) to produce a compound of formula (V) and hydrolysing said compound of formula (V). Also disclosed is a process of preparing a compound of (IV) (such as 20-ethyldihydrothevinone) which includes reacting thebaine with a compound such as 1-hexen-3-one to give 20-?-ethylthevinone, followed by a hydrogenation reaction. Also disclosed is a compound of formula (V) which is (S)-19-propyldihydrothevinol.
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