摘要 |
<p>NEW MATERIAL:DELTA<2>-Methanoprostacycline derivatives of formula I (R<1> is alkyl, alkenyl, phenoxymethyl; n is 0 and integral number of 1-6), their salts and their alkyl esters. EXAMPLE:6, 9-alpha-Methylene-11alpha, 15-dihydroxyprost-2-(E), 5, 13(E)-trienoic acid. USE:Remedy and preventive for thrombosis. They show stronger activity of inhibiting blood platelet coagulation than PGE1, and also have coronary vasodilating-and bronchodilating activities. PREPARATION:A selenium compound such as diphenyl selenide is made to act on a compound of formula II (R<2> is protecting group for carboxyl; R<3> is protecting group for hydoxyl) in a solvent such as THF or benzene in the presence of strong base at 0--70 deg.C and the product is treated with a peroxide such as 30% hydrogen peroxide to give a compound of formula III. Finally, the protecting groups are removed to form the compound of formula I.</p> |