NOVEL PROCESSES FOR THE PREPARATION OF PROSTAGLANDIN AMIDES

摘要

The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I,;where in the formula, the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5, 6 and 13, 14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.

主权项

1. Process for the preparation of the compounds of the general formula (IIA) where in the formula R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and n=0-3, characterized in that, a lactondiol of the general formula (XII), where the meanings of R3, Y and n are as defined above, is reduced into the lactoltriol of the general formula (XIII) where the meanings of R3, Y and n are as defined above, the protecting group of the compound of formula (XIII) is removed, and the resulting compound of the general formula (XIV), where the meanings of R3, Y and n are as defined above, is transformed by Wittig reaction into the compound of the general formula (IIA).