SMALL MOLECULE INHIBITORS OF MCL-1 AND USES THEREOF
申请人:THE REGENTS OF THE UNIVERSITY OF MICHIGAN
公开号:US20150284387A1
公开(公告)日:2015-10-08
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
Use of a secondary amine of formula I
R1-NH-R2
wherein R1 represents a branched alkyl group with 3 to 6 carbon atoms and R2 represents a hydrocarbon group comprising one or two ether groups
as blocking agent for compounds with at least one isocyanate group, hereinafter shortly referred to as isocyanates.
With the aid of a directing group, an imine moiety, heteroaromatic compounds add to acetylenes in the presence of a catalytic amount of [ReBr(CO)(3)(THF)](2) at the adjacent position of the directing group regioselectively to give hydroarylation of the acetylenes in good to excellent yields. Similarly, heteroaromatic compounds react with acrylates and isocyanates to give the corresponding hydroarylation products under rhenium catalysis. (C) 2008 Elsevier Ltd. All rights reserved.
A New Synthetic Method for the Preparation of Indenones from Aromatic Imines. Ru<sub>3</sub>(CO)<sub>12</sub>-Catalyzed Carbonylation at an <i>ortho</i> C−H Bond in the Aromatic Imines