Structure–activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes
摘要:
A variety of 2-oxoamides and related amides based on natural and non-natural amino acids were synthesized. Their activity on two human intracellular phospholipases (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase (GV sPLA(2)) was evaluated. We show that an amide based on (R)-gamma-norleucine is a highly selective inhibitor of GV sPLA2. (C) 2008 Elsevier Ltd. All rights reserved.
Cobalt-Catalyzed Asymmetric Markovnikov Hydroboration of Styrenes
作者:Xu Chen、Zhaoyang Cheng、Zhan Lu
DOI:10.1021/acscatal.8b05135
日期:2019.5.3
A cobalt-catalyzed asymmetric hydroboration of styrenes using an imidazoline phenyl picoliamide (ImPPA) ligand was first reported to deliver the valuable chiral secondary organoboronates with good functional tolerance and highenantioselectivity (up to >99% ee). This protocol is operationally simple without any activator. Particularly, this method can be applied in the asymmetric hydroboration of allylamine
The direct formation of functionalized alkyl(aryl)zinc halides by oxidative addition of highly reactive zinc with organic halides and their reactions with acid chlorides, .alpha.,.beta.-unsaturated ketones, and allylic, aryl, and vinyl halides
作者:Lishan Zhu、Richard M. Wehmeyer、Reuben D. Rieke
DOI:10.1021/jo00004a021
日期:1991.2
Highly reactive zinc, prepared by the lithium naphthalenide reduction of ZnCl2, readily undergoes oxidative addition to alkyl, aryl, and vinyl halides under mild conditions to generate the corresponding organozinc compounds in excellent yields. Significantly, the reaction will tolerate a spectrum of functional groups on the organic halides. Accordingly, this approach can now be used to prepare a wide variety of highly functionalized organozinc compounds. In the presence of Cu(I) salts, the organozinc compounds cross-couple with acid chlorides, conjugatively add to alpha,beta-unsaturated ketones, and regioselectively undergo S(N)2' substitution reactions with allylic halides. They also cross-couple with aryl or vinyl halides with Pd(0) catalysts.