Inhibitors of Acyl CoA:Cholesterol Acyltransferase
摘要:
Conformational restriction of previously disclosed acyclic diphenylethyl)diphenylacetamides led to the discovery of several potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). cis-[2-(4-Hydroxyphenyl)-1-indanyl]diphenylacetamide (4a) was the mo st potent ACAT inhibitor identified (IC50 = 0.04 mu M in an in vitro rat hepatic microsomal ACAT assay, ED(50) = 0.72 mg/kg/day in cholesterol-fed hamsters).
Iridium-Catalyzed Asymmetric Hydrogenation of Unfunctionalized Cycloalkenes to Access Chiral 2-Aryl Tetralins
作者:Tierui Pan、Qianjia Yuan、Defeng Xu、Wanbin Zhang
DOI:10.1021/acs.orglett.4c02054
日期:2024.7.12
The transition-metal catalyzed asymmetrichydrogenation of unfunctionalized alkenes is challenging. Herein, we report an efficient iridium-catalyzedasymmetrichydrogenation of unfunctionalized cycloalkenes, delivering chiral 2-aryl tetralins in excellent yields and with moderate to excellent enantioselectivities. The reaction can be performed on a gram-scale with a low catalyst loading (S/C = 1000)