| 摘要 |
<p>PURPOSE:To obtain a new PGE1 analog having platelet aggregationsuppressing action, more excellent in drug effect than a conventional prostaglandin (PG)F1 analog and reduced in side effects. CONSTITUTION:The objective PGE1 analog of formula I (R is H or 1-6C alkyl; A is vinylene or ethynylene) and its salt, e.g. (2E)-2,3,13,14-tetradehydro-PGE1- methyl ester. This compound can readily be produced from a compound of formula II (R<1> and R<2> are protecting group of OH) and a compound of formula III (R<3> is R excluding H) through a compound of IV to a compound of V. Furthermore, the compound of formula V can stereo-selectively be produced by reacting a compound of formula II with a compound of formula III and chlorotrimethylsilane in an inert solvent and then hydrolyzing the resultant compound of formula IV. The compound of formula I and its salt have strong platelet aggregation suppressing action and good long acting property of the action and hardly induce diarrhea at a dose capable of exhibiting sure pharmacological action. Therefore, the compound of formula I and its salt are useful for treatment for various kinds of diseases such as peripheral circulation disorder.</p> |
