发明名称 PROCESS FOR PREPARING ARYL- AND HETEROARYLACETIC ACID DERIVATIVES
摘要 The invention relates to a process for preparing aryl- and heteroarylacetic acids and derivatives thereof by reaction of aryl or heteroaryl halides with malonic diesters in the presence of a palladium catalyst, of one or more bases and optionally of a phase transfer catalyst. This process enables the preparation of a multitude of functionalized aryl- and heteroarylacetic acids and derivatives thereof, especially also the preparation of arylacetic acids with sterically demanding substituents.
申请公布号 US2014155632(A1) 申请公布日期 2014.06.05
申请号 US201214002691 申请日期 2012.02.27
申请人 Himmler Thomas;Goossen Lukas J.;Rudolphi Felix;Song Bingrui 发明人 Himmler Thomas;Goossen Lukas J.;Rudolphi Felix;Song Bingrui
分类号 C07D333/24;C07C253/30;C07C201/12;C07C67/343 主分类号 C07D333/24
代理机构 代理人
主权项 1. A process for preparing a compound of formula (III)in which Ar is agroup,where R1, R2, R3, R4 and R5 are the same or different and are each independently hydrogen, amino, cyano, nitro, halogen, optionally halogen-substituted C1-C6-alkyl, C1-C6-thioalkyl, thiophenyl, C1-C6-alkoxy, C6-C10-aryloxy, phenyl, —CO—C6-C10-aryl, —CO—C1-C3-alkyl, —COO—C1-C6-alkyl or —COO—C6-C10-aryl, the Ar radical may additionally also be a heteroaromatic radical or the Ar radical may also be 1- or 2-naphthyl, and R6 and R7 are each independently optionally substituted C1-C8-alkyl, phenyl, aryl, or NR8R9, where R8 and R9 are the same or different and are each independently C1-C4-alkyl, or phenyl optionally substituted by optionally fluorine- or chlorine-substituted C1-C3-alkyl, by nitro, cyano or di-C1-C3-alkylamino, or together with the nitrogen atom to which they are bonded are a saturated or unsaturated, substituted or unsubstituted cycle, wherein an aryl or heteroaryl halide of formula (I) Ar—Hal  (I)in which Hal is chlorine, bromine or iodine and Ar is as defined above, is reacted with a malonic ester of formula (II)in the presence of a palladium catalyst, of a phosphine ligand and A) of an inorganic base and of a phase transfer catalyst or B) of a mixture of inorganic bases, without using caesium carbonate or caesium bicarbonate, optionally using an organic solvent.
地址 Odenthal DE