| 摘要 |
NEW MATERIAL:The compound of formula I [R<1a> and R<2> are (substituted) 1-10C alkyl; R<3> is OH-protecting group or H; A is H and B is OH, or A and B together form a bond; X is H or halogen]. EXAMPLE:(4R)-5-[(1E)-6-methoxycarbonylhexylidene]-4-hydroxy-4- octyl-2-cyclo pentenone. USE:Pharmaceuticals. It has prostaglandin A-like structure, exhibits strong activity to inhibit the proliferation of cancer cells, and is expected to be useful as a carcinostatic agent. PREPARATION:The compound of formula I wherein A is H and B is OH can be prepared by carrying out the aldol condensation reaction of the 4-hydroxy-2- cyclopentenone compound of formula II with the aldehyde of formula III in a solvent in the presence of a basic compound, and if necessary, subjecting the product to the deprotection, hydrolysis, etc. Another compound of formula I wherein A and B together form a bond (the configuration of R<1> is E or Z) is obtained by the dehydration reaction of the above product. |
