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Process for the preparation of pleuromutilins
专利权人:
NABRIVA THERAPEUTICS AG
发明人:
RIEDL ROSEMARIE,HEILMAYER WERNER,SPENCE LEE
申请号:
NZ60380411
公开号:
NZ603804A
申请日:
2011.05.23
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
603804 Process for the preparation of a Compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a Compound of formula IIa or in a mixture of a compound of formula IIa With a compound of formula IIb and isolating a Compound of formula I from the reaction mixture; Compounds and salts of Compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a Compound of formula I. some of the exemplified compounds of formula I include: 14-O-{ [(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl} -mutilin acetate in crystalline Form A; 14-O-{ [(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl} -mutilin acetate in crystalline Form B 14-O-{ [(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl} -mutilin L-Iactate in crystalline Form 1, and 14-O-{ [(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl} –mutilin hydrogenmaleate in crystalline Form 1.
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