Borane-Catalyzed Reductive α-Silylation of Conjugated Esters and Amides Leaving Carbonyl Groups Intact
作者:Youngchan Kim、Sukbok Chang
DOI:10.1002/anie.201508669
日期:2016.1.4
valuable α‐silyl carbonyl products. The α‐silylation occurs chemoselectively, thus leaving the labile carbonylgroups intact. The reaction features a broad scope of both acyclic and cyclic substrates, and the synthetic utility of the obtained α‐silyl carbonyl products is also demonstrated. Mechanistic studies revealed two operative steps: fast 1,4‐hydrosilylation of conjugated carbonyls and then slow
本文描述了由B(C 6 F 5)3催化的α,β-不饱和酯和酰胺的氢化硅烷化反应,以提供具有合成价值的α-甲硅烷基羰基产物。α-甲硅烷基化是化学选择性发生的,因此保留了不稳定的羰基。该反应具有无环和环状底物的广泛范围,并且还证明了所得α-甲硅烷基羰基产物的合成效用。机理研究揭示了两个操作步骤:共轭羰基的快速1,4-氢化硅烷化,然后减慢甲硅烷基醚中间体的甲硅烷基迁移。
Thiazepinyl hydroxamic acid derivatives as matrix metalloproteinase inhibitors
申请人:——
公开号:US20030134849A1
公开(公告)日:2003-07-17
A compound of formula (I) in which R
1
is halo, lower alkoxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted heterecyclic group or optionally substituted lower alkynyl, R
2
is amidated carboxy, R
3
is hydrogen or acyl, Ar is aryl or heterocyclic group, X is thia, sulfinyl or sulfonyl, Y and Z are each lower alkylene, m and n are each an integer of 0 to 2, and a salt thereof, useful as inhibitors of matrix metalloproteinases (MMP) or the production of tumor necrosis factor &agr; (TNF &agr;).
[EN] THIAZEPINYL HYDROXAMIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] DERIVES DE L'ACIDE THIAZEPINYLHYDROXAMIQUE EN TANT QU'INHIBITEURS DES METALLOPROTEINASES MATRICIELLES
申请人:FUJISAWA PHARMACEUTICAL CO
公开号:WO2001060808A1
公开(公告)日:2001-08-23
A compound of formula (I) in which R1 is halo, lower alkoxy, optionally substituted aryl, optionally substituted aryloxy, optionally substituted heterecyclic group or optionally substituted lower alkynyl, R2 is amidated carboxy, R3 is hydrogen or acyl, Ar is aryl or heterocyclic group, X is thia, sulfinyl or sulfonyl, Y and Z are each lower alkylene, m and n are each an integer of 0 to 2, and a salt thereof, useful as inhibitors of matrix metalloproteinases (MMP) or the production of tumor necrosis factor α (TNF α).
Compounds for treatment of inflammation, diabetes and related disorders
申请人:——
公开号:US20040097593A1
公开(公告)日:2004-05-20
Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.
COMPOUNDS FOR TREATMENT OF INFLAMMATION, DIABETES AND RELATED DISORDERS
申请人:Neogi Partha
公开号:US20070259961A9
公开(公告)日:2007-11-08
Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory diseases, immunological diseases and cancer.