| 摘要 |
<p>PURPOSE:To facilitate the removal of by-products under mild conditions and obtain the pyrimidine derivative having inhibiting activities against 3-hydroxy-3- methylglutaryl coenzyme A (HMG-CoA) reductases by reacting a specific aldehyde compound with a specified ketophosphonate in the presence of a base in an organic solvent. CONSTITUTION:This process for producing a pyrimidine derivative expressed by formula III (R<1> is an alkyl, a cycloalkyl, an aryl or amino; R<2> and R<3> are each H, an alkyl, a cycloalkyl or phenyl; R<4> is H or carboxy-protecting group; R<5> is H or a hydroxy-protecting group] is to react an aldehyde compound expressed by formula I [X is N or R<6>C (R<6> is an alkyl, or, together with the adjacent C may form a condensed benzene ring)] with a ketophosphonate derivative expressed by formula II (R<7> and R<8> are each an alkoxy) in the presence of a base in an organic solvent such as toluene at about ambient temperature. An HMG-CoA reductase inhibitor which is a central enzyme for biosynthesis of cholesterol can safely be produced in a high yield according to the method for production. This process is advantageous due to the use of the ketophosphonate derivative having high reactivity and by-products can readily be removed due to their water solubility.</p> |
