| 摘要 |
<p>PURPOSE:To obtain a PGE derivative in a simplified reaction system in good yield by reacting 4-substituted-2-cyclopenten-1-ones with an organozinc compound and then an unsaturated compound. CONSTITUTION:A compound expressed by formula I (R<1> is H or protecting group of OH) is reacted with an organozinc compound obtained from an organolithium compound expressed by formula II (R<2> is H or protecting group of OH; R<3> is single bond or 1-4C alkylene; R<4> is 1-7C alkyl, 4-7C cycloalkyl, etc.; D is cis- or trans-vinylene), a zinc compound expressed by the formula Zn-(X1)2 (X1 is halogen) and methyllithium. The resultant product is then reacted with an unsaturated compound expressed by formula III (X2 is halogen, tosyl or mesyl; A is trans- or cis-vinylene or ethynylene; R<5> is H, 1-4C alkyl or 4-7C cycloalkyl, etc.) to afford a PGE derivative expressed by formula IV. The reaction is carried out in an aprotic inert organic solvent (e.g. THF) at -100 to +20 deg.C.</p> |
