| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a new compound capable of remarkably inhibiting proliferation of human capillary endothelial cell and extremely useful as an arterialization inhibitor. SOLUTION: This compound is a 2-acylaminobenzamide derivative of formula I R<1> is H, a halogen, etc.; R<2> and R<3> are each H, a lower alkyl, etc.; B is N(R<4> )(R<5> ) (R<4> and R<5> are each H, a lower alkyl, etc.), NH-(CH2 )n -A-R<6> [A is a single bond, etc.; R<6> is a substitutable amino; (n) is 2-6]} or its salt, e.g. (E)-2-(3,4-dimethoxycinnamoylamino)benzamide. The compound of formula I is obtained by reacting a carboxylic acid derivative of formula II (R<10> is H, a halogen, etc.) or its reactive functional derivative such as its acid halide or active ester with a 2-acylaminobenzamide derivative, etc., of formula III [B<0> is N(R<4> )(R<5> ), etc.] and a dehydrating agent or a condensation agent in an inert solvent in the presence of a base and as necessary, eliminating a protective group and hydrolyzing the reaction product.</p> |
