79363-73-8Relevant articles and documents
Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease
Li, Xianfeng,Zhang, Yong-Kang,Liu, Yang,Ding, Charles Z.,Li, Qun,Zhou, Yasheen,Plattner, Jacob J.,Baker, Stephen J.,Qian, Xuelei,Fan, Dazhong,Liao, Liang,Ni, Zhi-Jie,White, Gemma V.,Mordaunt, Jackie E.,Lazarides, Linos X.,Slater, Martin J.,Jarvest, Richard L.,Thommes, Pia,Ellis, Malcolm,Edge, Colin M.,Hubbard, Julia A.,Somers, Don,Rowland, Paul,Nassau, Pamela,McDowell, Bill,Skarzynski, Tadeusz J.,Kazmierski, Wieslaw M.,Grimes, Richard M.,Wright, Lois L.,Smith, Gary K.,Zou, Wuxin,Wright, Jon,Pennicott, Lewis E.
, p. 3550 - 3556 (2010)
We have designed and synthesized a novel series of α-amino cyclic boronates and incorporated them successfully in several acyclic templates at the P1 position. These compounds are inhibitors of the HCV NS3 serine protease, and structural studies show that they inhibit the NS3 protease by trapping the Ser-139 hydroxyl group in the active site. Synthetic methodologies and SARs of this series of compounds are described.
Preparation of 2-oxygen derivatives of 1,2-oxaborolane from 2-allyloxy-1,2-oxaborolane
Weike, Zhou,Weiming, Lo,Gaoyi, Zhang,Hongxun, Ding,Shaofang, Liang
, p. 131 - 146 (2007/10/02)
2-Allyloxy-1,2-oxaborolane (V), readily obtained by hydroboration of allyl alcohol with borane reagents such as KBH4-HOAc, was used as a key reactant in the synthesis of a series of 2-oxygen derivatives of 1,2-oxaborolane. 2-Allyl-1,2-oxaborolane (XXIII) and 2-hydro-1,2-oxaborolane dimethylsulfide complex (XXIV), prepared from the reaction of V with allylmagnesium bromide and dimethylsulfideborane complex (BMS) respectively, were also used as the reactive intermediates for some of the lower 2-alkyloxy-1,2-oxaborolanes.Five procedures and other probable routes from V to 2-oxygen derivatives of 1,2-oxaborolane are described.
