Rhodium(III)-Catalyzed Indazole Synthesis by C–H Bond Functionalization and Cyclative Capture
摘要:
An efficient, one-step, and highly functional group-compatible synthesis of substituted N-aryl-2H-indazoles is reported via the rhodium(III)-catalyzed C-H bond addition of azobenzenes to aldehydes. The regioselective coupling of unsymmetrical azobenzenes was further demonstrated and led to the development of a new removable aryl group that allows for the preparation of indazoles without N-substitution. The 2-aryl-2H-indazole products also represent a new class of readily prepared fluorophores for which initial spectroscopic characterization has been performed.
Light to dissolve: (R)‐ and (S)‐diamides bearing a hydrogen‐bonding framework (red in picture) and a trans‐azobenzene unit (blue) form an insoluble heterochiral aggregate, which can be dissolved by photoisomerization of the azobenzene unit to the cis conformation by UVirradiation (365 nm). The insoluble aggregate was formed again by subsequent irradiation with visible light (>422 nm). The precipitation
Novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, enantiomers thereof or prodrugs thereof of Formula (I)
wherein the substituents are as defined herein, which are useful as therapeutic agents.
Benzenesulfonamide Compounds and Their Use as Blockers of Calcium Channels
申请人:Chen Zhengming
公开号:US20100022595A1
公开(公告)日:2010-01-28
The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R
1
-R
3
, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.