| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a new compound having a chymase-inhibiting activity, capable of being permitted as an active ingredient for medicines, and useful for treating and preventing cardiac and circulatory disorders. SOLUTION: A compound of formula I [R<1> is H, an amino-protecting group; R<2> is an ar(lower)alkyl; R<3> is a halogen-substituted lower alkyl, etc.; X is a group of formula II (R<4> is a halogen, a lower alkoxy, etc.), etc.; Z is N or CH); Y is a lower alkylene] and its salt. For example, 2-[5-[(Benzyloxycarbonyl) amino]-2-phenyl-1,6-dihydro-6-oxo-1-pyrimidinyl]-N-[2-(4,4,4-trifluoro -3-hydroxy-1- phenyl)butyl]acetamide. The new compound of formula I, especially a compound of formula IV, is obtained by reacting a compound of formula III or its salt with an oxidizing agent (e.g. potassium permanganate) in a solvent not affecting the reaction, such as water or an organic solvent, in a somewhat mild state.</p> |
