Process for the preparation of prostaglandin analogues

C - Chemistry – Metallurgy – 08 – B

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260/235.03

C08B 37/16 (2006.01) C07C 405/00 (2006.01) C07D 309/12 (2006.01) C08B 37/00 (2006.01)

Patent

CA 1098124

ABSTRACT The present invention relates to prostaglandin analogues of the general formula:- Image wherein X represnts cis or trans-vinylene or ethylene, Z represents Image or Image , R1 represents a hydrogen atom or a straingh- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R2 represents a hydrogen atom or a methyl group. R3 represents a straight- or branched-chain alkylene group containing from 1 to 7 carbon atoms and R4 represents a cycloalkyl group containing from 5 to 7 carbon atoms, a grouping of the formula:- Image (wherein R5 and R6, which may be the same or different, each represent a hydrogen atom or halogen atom, a trifluoromethyl group of a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms), or a grouping of the formula:- Image (wherein R5 and R6 are as hereinbefore defined), or R3 and R4 together represent a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and (1) the double bond between C3-C4 is trans or cis or trans and cis, when X is cis-vinylene or ethylene, and (2) the double bond between C3-C4 is trans, when X is trans-vinylene, and the double bond between C13-C14 is trans with the exclusion of these prostaglandin analogues wherein X represents cis-vinylene or ethylene, Z represents Image , R1 and R2 represent hydrogen atoms, R3 and R4 together represent n-pentyl and the double bond between C3-C4 is trans) and cyclodextrin clathrates of such acids and esters, and when R1 represents a hydrogen atom, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.

273659

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