Preparing water-soluble probucol derivative, useful as cholesterol reducing agent, comprises reacting probucol compound with aliphatic saturated dicarboxylic acid, maleic acid or phthalic acid, in presence of a magnesium compound

摘要

Preparation of water soluble probucol derivative (I) or its salt comprises reacting a probucol compound (II) with anhydrides of aliphatic saturated dicarboxylic acid (IIIa), maleic acid or phthalic acid, in the presence of a magnesium compound (IV). Preparation of water soluble probucol compound of formula (I) comprises reacting a probucol compound of formula (II) with anhydrides of aliphatic dicarboxylic acid of formula HO-(O)C-(CH2)n-C(O)-OH (IIIa), maleic acid or phthalic acid, in the presence of a magnesium compound of formula R7-Mg-Hal (IV). R1-R41-4C alkyl such as methyl or tert.butyl (preferred); R5, R61-8C alkenyl, phenyl or preferably 1-8C alkyl such as methyl; A : a group of aliphatic carboxylic acid (IIa) of formula -C(O)-(CH2)n-C(O)-OH, unsaturated carboxylic acid (IIb) of formula -C(O)-CH=CH-C(O)-OH or ortho substituted aromatic carboxylic acid (IIc) of formula (-C(O)-C6H4(ortho)-C(O)OH); Bx : H or A; n : 1-6 (preferably 2); R71-12C alkyl or phenyl; and Hal : halo. [Image].