发明授权
US07777056B2 Method for manufacture of 4-hydroxy pyran-2-one derivatives 有权
4-羟基吡喃-2-酮衍生物的制备方法

Method for manufacture of 4-hydroxy pyran-2-one derivatives
摘要:
A process for preparation of 4-hydroxy-pyran-2-one derivative of formula (I), wherein R is, and wherein R1 and R2 are methyl and R3 is hydrogen or methyl, comprising the steps of, heating a compound of formula (II), wherein R is as defined before, and R4 is hydrogen, NH4+ or an alkali metal, in a solvent mixture consisting of an aromatic hydrocarbon and a ketone in an inert atmosphere at a temperature of between 60° C. to 92° C. in the absence or presence of orthophosphoric acid or its alkali dihydrogen salts or alkali hydrogen salts of a dibasic acid, followed by optional neutralization of the reaction mixture with an organic base and obtaining compound of formula (I) in high purity and substantially free of impurities through a step of isolation and crystallization. The process leads to formation of derivatives of formula I in high purity with dimmer impurity (III) less than 0.1% and anhydro impurity (IV) below 0.15%.
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