| 摘要 |
PURPOSE:To provide a new pyrimidine derivative useful as a 3-hydroxy-3- methylglutaryl coenzyme A reduction inhibitor, thus effective for the therapies of hypercholesterolemia, hyperlipoproteinemia, and also atherosclerosis. CONSTITUTION:The objective compound of formula I (R<1> is lower alkyl, aryl or aralkyl; R<2> and R<3> are each H, alkyl or aryl; R<4> is H, alkyl or cation capable of forming nontoxic, pharmaceutically permissible salt; X is sulfur, oxygen, sulfonyl or imino) or cyclized lactone compound therefrom, for example, sodium (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N- methylsulfonylaminopyrimidin)-5-yl] (3R, 5S)-dihydroxy-(E)-6-heptenoate. The compound of the formula I can be obtained by producing, starting from a compound of formula II, a compound of formula III followed by a compound of formula IV and then a compound of formula V which is, in turn, made to react with diethylmethoxyborane and NaBH4). |
