METHOD OF PREPARING 4-OXO-PGI2 AND ANALOGUES THEREOF

摘要

1. Optically active and racemic 4-oxo-PGI2 derivatives of general formula I see diagramm : EP0063338,P15,F3 wherein Q represents a -COOR**1 , -CH2 -OH, -COL**1 group, wherein R**1 represents a hydrogen atom, an alkali metal, alkaline earth metal or aluminium cation, an ammonium or tris-hydroxymethyl-ammonium ion, C1-6 alkyl, C3-10 cycloalkyl, C1-4 alkyl which is substituted by unsubstituted phenyl or by phenyl substituted by halogen, phenyl, C1-4 alkyl or by halogen-substituted C1-4 alkyl, or phenyl which may be substituted by halogen, phenyl, C1-4 alkyl or halogen-substituted C1-4 alkyl, L**1 represents amino, C1-6 alkylamino or Di-C1-6 -alkylamino, X represents -CH2 -CH2 -, -CH=CH-, -CH2 -C(CH3 )2 -, -(CH3 )2 C-CH2 - or cyclopropylene, A represents trans- or cis-CH=CH-, -C-=C-, or -CH2 -CH2 -, R**2 represents a hydrogen atom with alpha- or beta-configuration, methyl or ethyl, R**3 represents a hydrogen atom, C1-4 -alkanoyl, benzoyl which may be substituted by halogen, phenyl, C1-4 alkyl or halogen substituted C1-4 alkyl, or a tri-C1-4 -alkylsilyl protecting group, R**4 and R**5 , independently of each other, represent a hydrogen atom or C1-4 alkyl, B represents methylene, oxygen or -NH- and R**6 represents C1-6 alkyl, phenyl which may be substituted by halogen, phenyl, C1-4 alkyl or halogen-substituted C1-4 alkyl.