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A significantly improved synthesis of 5,8-difluoro-2H-chromene 1 using silicone oil as the reaction solvent is described. The new method eliminated the tedious workup and large quantity of waste produced via conventional methods. To our best knowledge, this is the first report of conducting an organic reaction using silicone oil as an organic solvent.

The title imidazo[1,2-a]pyridines (V), (VIII), (XI) are obtained by Ga(OTf)3- catalyzed reaction of various primary heterocyclic amidines and isocyanides.

The atropisomeric properties observed in case of products obtained by the transformation of 2-amino-5-haloheterocycles, 2-isocyanophenyl acetate and aryl aldehydes equipped with electron-withdrawing substituents is examined.

The synthesis of cyclazines involves initial three-component condensation and a Pd-catalyzed intramolecular α-arylation of an α-aminocarbonyl functionality.

Some of the synthesized compounds exhibit relatively strong cytotoxicity against the HeLa cell line.

We recently discovered and reported a novel series of benzhydrylpiperazine derivatives bearing an asymmetric carbon atom that are potent and selective hCB1 inverse agonists. In the present study, we used Davis-Ellmann-type sulfonamide chemistry to asymmetrically synthesize two enantiomers of the most potent racemic N-cyclohexyl-4-[1-(2,4-dichlorophenyl)-1-(p-tolyl)methyl]piperazine-1-carbo-xamide [14] . Enantiomer separation and configuration assignment were carried out. Our results indicate that the R-configuration is the more active enantiomer, displaying enhanced antagonistic activity for hCB1 receptor, better oral bioavailability, and greater efficacy in the reduction of body weight in diet-induced obese mice.

A variety of ketoximes (I) reacts to the corresponding amides (II) under optimized and mild conditions.

The conditions of the intramolecular Goldberg reaction [CuI/N,N-dimethylglycine] are successfully applied to the synthesis of the title compounds (VIII).

The present study describes the identification via privileged structure-based approach of the benzhydrylpiperazine moiety as a potential scaffold to develop novel CB(1) receptor modulators. Efficient structural optimization of the initial four hit compounds led to a high quality lead series, represented by compound 6c. Compound 6c is a highly potent and selective CB(1) receptor inverse agonist that is able to reduce body weight in diet-induced obese Sprague-Dawley rats. The preparation of privileged structure-based library, the progression from hit to lead, the structure-activity relationships in the lead series and in vitro and in vivo activity of compound 6c are discussed.