| 摘要 |
<p>PURPOSE:To obtain a new intermediate useful as a synthetic intermediate for dihalogenated prostacyclines exhibiting strong physiological activity in vivo and having high chemical stability. CONSTITUTION:This intermediate is a compound of formula I [Q is a (substituted)1-10C alkyl, a (substituted)1-10C alkenyl, etc.; R<4> and R<5> are each independently H,5p a protecting group; X<1> and X<2> are each independently a halogen, preferably fluorine atom], e.g. (1S,5R,6R,7R)-2-oxa-4-fluoro-7-(2- tetrahydropyranyloxy)-6-hydroxymethyl-bicyclo[3,3,0]octan-3-one. The compound of formula I can efficiently and practically be produced by dehydrating an addition reaction product of a dihalogenated lactone of formula II with an organometallic compound of formula III (M is a metal atom; L is a metal ligand; (m) is an integer of 1-8; (n) is an integer of 0-10). This group Q is preferably group of formula B-Z (B is a 1-6C alkylene, etc.; Z is carboxyl, formyl, etc.).</p> |
