已经开发出一种温和、催化、原子经济的咪唑并[1,2- a ]吡啶合成方法:催化二氯(2-吡啶羧基)金[PicAuCl 2 ]在酸存在下产生一系列咪唑并[1,2- a ]吡啶以炔烃和 2-氨基吡啶N-氧化物为起始原料,收率良好。这种策略是温和的,预计特别适用于在咪唑并[1,2- a ]吡啶环附近安装立体中心,而不损失对映体过量。
Gold-Catalyzed Redox Synthesis of Imidazo[1,2-<i>a</i>]pyridines using Pyridine<i>N</i>-Oxide and Alkynes
作者:Eric P. A. Talbot、Melodie Richardson、Jeffrey M. McKenna、F. Dean Toste
DOI:10.1002/adsc.201300996
日期:2014.3.10
synthesis of imidazo[1,2‐a]pyridines has been developed: catalytic dichloro(2‐pyridinecarboxylato)gold [PicAuCl2] in the presence of an acid produces a range of imidazo[1,2‐a]pyridines in good yields starting from alkynes and 2‐aminopyridine N‐oxides. This strategy is mild and foreseen to be of particular use for the installation of stereogenic centers adjacent to the imidazo[1,2‐a]pyridine ring without
已经开发出一种温和、催化、原子经济的咪唑并[1,2- a ]吡啶合成方法:催化二氯(2-吡啶羧基)金[PicAuCl 2 ]在酸存在下产生一系列咪唑并[1,2- a ]吡啶以炔烃和 2-氨基吡啶N-氧化物为起始原料,收率良好。这种策略是温和的,预计特别适用于在咪唑并[1,2- a ]吡啶环附近安装立体中心,而不损失对映体过量。
Substituted phenylalkanoic acids and derivatives
申请人:Yoshitomi Pharmaceutical Industries, Ltd.
公开号:US03978071A1
公开(公告)日:1976-08-31
Substituted phenylalkanoic acids and derivatives thereof of the formula: ##SPC1## Wherein each of R.sup.1 and R.sup.2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; each of X.sup.1 and X.sup.2 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; Y is COOH, COOR (wherein R is an alkyl group having 1 to 4 carbon atoms), CONH.sub.2, CSNH.sub.2, CN or COZ--A--N(R.sup.3)(R.sup.4) (wherein Z is an oxygen atom or an imino group, A is an alkylene group having 2 to 4 carbon atoms and each of R.sup.3 and R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form a saturated heterocycle selected from pyrrolidine, piperidine, morpholine, piperazine and piperazine substituted by an alkyl group having 1 to 4 carbon atoms at the 4-position; and ring P represents a pyridine ring, a pyrimidine ring or a thiazole ring; and pharmaceutically acceptable salts thereof are useful as analgesics, anti-pyrestics and anti-inflammatory agents.