发明授权
- 专利标题: Method for manufacture of 4-hydroxy pyran-2-one derivatives
- 专利标题(中): 4-羟基吡喃-2-酮衍生物的制备方法
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申请号: US11547533申请日: 2004-03-30
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公开(公告)号: US07777056B2公开(公告)日: 2010-08-17
- 发明人: Milind Moreshwar Gharpure , Swapnil Panditrao Sonawane , Srihari Shivaji Mane , Rajendra Dagesing Mahale
- 申请人: Milind Moreshwar Gharpure , Swapnil Panditrao Sonawane , Srihari Shivaji Mane , Rajendra Dagesing Mahale
- 申请人地址: IN Mumbai
- 专利权人: Lupin Ltd.
- 当前专利权人: Lupin Ltd.
- 当前专利权人地址: IN Mumbai
- 代理机构: Merchant & Gould P.C.
- 国际申请: PCT/IN2004/000075 WO 20040330
- 国际公布: WO2005/095374 WO 20051013
- 主分类号: C07D311/02
- IPC分类号: C07D311/02
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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