16076-61-2Relevant academic research and scientific papers
Remote ester group leads to efficient kinetic resolution of racemic aliphatic alcohols via asymmetric hydrogenation
Yang, Xiao-Hui,Wang, Ke,Zhu, Shou-Fei,Xie, Jian-Hua,Zhou, Qi-Lin
supporting information, p. 17426 - 17429 (2015/02/02)
A highly efficient method for kinetic resolution of racemic aliphatic alcohols without conversion of the hydroxyl group has been realized; the method involves hydrogenation mediated by a remote ester group and is catalyzed by a chiral iridium complex. This powerful, environmentally friendly method provides chiral δ-alkyl-δ-hydroxy esters and δ-alkyl-1,5-diols in good yields with high enantioselectivities even at extremely low catalyst loading (0.001 mol %).
Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors
Barnes-Seeman, David,Boiselle, Carri,Capacci-Daniel, Christina,Chopra, Rajiv,Hoffmaster, Keith,Jones, Christopher T.,Kato, Mitsunori,Lin, Kai,Ma, Sue,Pan, Guoyu,Shu, Lei,Wang, Jianling,Whiteman, Leah,Xu, Mei,Zheng, Rui,Fu, Jiping
, p. 3979 - 3985 (2014/11/08)
Herein we report the successful incorporation of a lactam as an amide replacement in the design of hepatitis C virus NS5B Site II thiophene carboxylic acid inhibitors. Optimizing potency in a replicon assay and minimizing potential risk for CYP3A4 induction led to the discovery of inhibitor 22a. This lead compound has a favorable pharmacokinetic profile in rats and dogs.
