2,6-Pyridine di:methanol bis(3,4,5-trimethoxybenzoate) prepn. - by trans-esterification of 2,6-pyridine di:methanol with 3,4,5-tri:methoxy benzoic acid ester in presence of base

摘要

Pyridine-2,6-dimethyl bis-(3,4,5-trimethoxybenzoate) of formula (I) is new. (I) is an antiatherogenic agent with high activity in reducing total aortic cholesterol, with an increase in free cholesterol/esterified cholesterol ratio. (I) is obtd. by reacting 2,6-bis-(hydroxymethyl) pyridine (II) with a 3,4,5-trimethoxybenzoic acid ester in presence of a base, e.g. in a 1:2.2 molar ratio in presence of NaH at about 130 deg.C. then at 160-170 deg.C. after addn. of ester, with reaction for 6-12 hrs. (I) is obtd. in 70-90% yield and high purity. (Provisional Basic previously advised in Week 8347).