Visible-Light Photoredox-Catalyzed Intermolecular α-Aminomethyl/Carboxylative Dearomatization of Indoles with CO<sub>2</sub> and α-Aminoalkyl Radical Precursors
作者:Wanxu Gao、Qi Yang、Han Yang、Yang Yao、Junxue Bai、Jianwei Sun、Song Sun
DOI:10.1021/acs.orglett.3c03755
日期:2024.1.19
α-aminomethyl/carboxylative dearomatization of indoles with CO2 and α-aminoalkyl radical precursors, affording a series of functionalized indoline-3-carboxylic acids and lactams in good yields with high regioselectivity. This multicomponent reaction provides a green and facile method for the synthesis of diverse functionalized indolines by using CO2 as the carboxylic and carbonyl source.
Biphenylylglycine derivatives and their salts with bases
申请人:Chugai Seiyaku
Kabushiki Kaisha
公开号:EP0003847A1
公开(公告)日:1979-09-05
Biphenylylglycine derivatives of the general formula I
wherein Ri is an amino group or a protected amino group and their salts with bases. The compounds are useful as intermediates for synthesizing various penicillin and cephalosporin derivatives which have excellent antibacterial activities. The compounds can be prepared, for example, by reacting an N-substituted-a-hydroxy-glycine with o,o'- dihydroxybiphenyl in the presence of an acid catalyst in an inert organic solvent. The compounds contain an asymmetric carbon atom at the a-position to the carboxy group. The invention covers the racemic mixtures and the D- and L-isomers.
通式 I 中 Ri 为氨基或受保护氨基的联苯甘氨酸衍生物及其碱式盐。 这些化合物可用作合成各种青霉素和头孢菌素衍生物的中间体,这些衍生物具有优异的抗菌活性。 例如,可在惰性有机溶剂中,在酸催化剂存在下,通过使 N-取代-a-羟基甘氨酸与 o,o'- 二羟基联苯反应制备这些化合物。 这些化合物在 a 位与羧基之间含有一个不对称碳原子。 本发明包括外消旋混合物以及 D-和 L-异构体。
HOMOCYSTEINE SYNTHASE INHIBITOR
申请人:Mitsubishi Tanabe Pharma Corporation
公开号:EP2275404A1
公开(公告)日:2011-01-19
The present invention aims to provide a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase.
The present invention relates to use of a compound represented by the following formula (I)
wherein each symbol is as defined in the DESCRIPTION, or a pharmacologically acceptable salt thereof, or a solvate thereof as a homocysteine synthase inhibitor.