Design and synthesis of boronic acid inhibitors of endothelial lipase
摘要:
Endothelial lipase (EL) and lipoprotein lipase (LPL) are homologous lipases that act on plasma lipoproteins. EL is predominantly a phospholipase and appears to be a key regulator of plasma HDL-C. LPL is mainly a triglyceride lipase regulating (V)LDL levels. The existing biological data indicate that inhibitors selective for EL over LPL should have anti-atherogenic activity, mainly through increasing plasma HDL-C levels. We report here the synthesis of alkyl, aryl, or acyl-substituted phenylboronic acids that inhibit EL. Many of the inhibitors evaluated proved to be nearly equally potent against both EL and LPL, but several exhibited moderate to good selectivity for EL. (C) 2011 Elsevier Ltd. All rights reserved.
An improved process for preparing diarylamines from alicyclic ketones, a primary aromatic amine, and a hydrogen acceptor, in the presence of a platinum metal catalyst and an acid promoter.
一种改进的工艺,在铂金属催化剂和酸促进剂存在下,由脂环酮、芳香族伯胺和氢受体制备二芳基胺。
Method for preparing aromatic secondary amino compound
申请人:MITSUI TOATSU CHEMICALS, Inc.
公开号:EP0588060A2
公开(公告)日:1994-03-23
[Constitution] A method for preparing diphenylamine from cyclohexanone and aniline by adding dropwise nitrobenzene and cyclohexanone to a reaction system in which a hydrogen transfer catalyst and a sulfur-free polar solvent are present and aniline is being formed from nitrobenzene as a hydrogen acceptor.
[Effect] Diphenylamine can be obtained in a high yield under moderate reaction conditions.