Shin-ichi Yamada

An improved method for the introduction of carbon-carbon triple bond at C-13 in PG synthesis

Abstract An improved method for the introduction of carbon-carbon triple bond at C-13 in PG-synthesis is described. The efficient aldol reaction of aldehydes has been achieved by using α-chloro enolate anions derived from 1-bromo-1-chloro ketones, giving α-chloro enones after dehydration in good yields, the precursor of the acetylenic alcohols.

Syntheses and biological activities of chemically stable prostacyclin mimics with cis-bicyclo[4.3.0]nonene ring system: the novel homoisocarbacyclin analogues.

The synthetic studies concerning a series of homoisocarbacyclin analogues, which are homologous compounds of isocarbacyclin, with cis-bicyclo[4.3.0]non-2-ene or cis-bicyclo[4.3.0]non-3-ene as a nucleus have been carried out. The general synthetic methods of homoisocarbacyclin analogues have been accomplished starting with the versatile Corey lactone. Among the analogues synthesized in the present studies, a promising compound (TY-11223) exhibiting a good selectivity in biological actions was found to be studied further.