| 摘要 |
<p>PURPOSE:To obtain the subject new compound having a combination of excellent lipid peroxide formation-inhibitory activity and protein-stabilizing activity, thus useful as a therapeutic agent for cataract. CONSTITUTION:The objective compound is expressed by formula I {R<1> is (protected) OH; R<2> is a lower alkyl; R<3> is H, a [(protected) OH- or (protected) (lower alkyl)amino-substituted] lower alkyl- or (protected) lower alkoxyl; R<4> is a (ester- or amide-converted) carboxyl, tetrazol-yl, (ester- or amide-converted) phosphone, etc.; A is an alkylene; B is C=O, C=S or CH2} or a salt thereof, e.g. 2-(3,5-di-t-butyl-4-hydroxybenzylidene)-4-phosphonomethylthiomorpholin -3-one. The compound of formula I (where, R<1> is OH; R<4> is carboxyl) is obtained by the following processes: a compound of formul.a II is reacted with a compound of formula III in the presence of a base to form a compound of formula IV followed by protecting its OH group and then reaction with a compound of formula, VY-A-R<4> (Y is a halogen, etc.) in the presence of a base followed by eliminating the OH-protecting group.</p> |
