A new and efficient preparation of pharmacologically and biologically important 2,5-disubstituted 6-azaindoles was achieved from cyclizations of aziridin-2-yl dipropargylic alcohols as adducts of two propargyl groups to ethyl 1-benzylaziridine-2-carboxylate. The sequential cyclizations include pyrrole formation and a novel base-catalyzed intramolecular acetylenic Schmidt reaction.

Cyclin dependant kinase-2 (CDK-2) is a key regulator of cell cycle progression and glycogen synthase kinase-3 (GSK3) that plays a critical role in the regulatory pathway of serine/threonine kinase, which is being targeted for the treatment of human cancer. The natural product of 1, 2 disubstituted idopyranose (C23H28O12) was isolated from the leaves of the medicinal plant, Vitex negundo to trea...

In this article, simple, convenient synthesis of 2-aryl-1- arylmethyl-1H-1,3-benzimidazole (1,2-disubstituted benzimidazoles) via condensation of 1,2-phenylenediamine and aromatic aldehydes using SBA-Pr-SO3H as a nanoporous solid acid catalyst in green protocol was reported.

A novel series of optically active 2,6-disubstituted alkylphenols with improved anesthetic profiles compared to widely used propofol were synthesized. The incorporation of the cyclopropyl group not only increased the steric effect but also introduced stereoselective effects over their anesthetic properties. Compounds 1, 2, and 6 were selected as potential candidates for further preclinical deve...

The first access to N-1, N-4 disubstituted pyrrolo[2,3-d][1,2,3]triazoles is reported. series were generated using a “one-pot” MCR, leading single regioisomer of the attempted heteroaromatic skeleton in good yields. Next, functionalization C-5 and C-6 positions was investigated. (Het)aryl groups introduced at regioselective electrophilic brominations followed by Suzuki–Miyaura cross coupling re...

Treating 2-chloro-4-(4-chlorophenyl)-6-methylbenzo[d]-3,1-oxazinium hexachloroantimonate (1) with one equivalent of alcohol or mercaptane led, after hydrolysis with aq. NaOH, to the formation of 4,4-disubstituted-1,4-dihydro-2H-6-methyl-3,1-benzoxazin-2-ones (3). Large excess addition of alcohol afforded either 4’-chloro-2-isocyanato-5-methylbenzophenone disubstitutedketal (4) or N-{2[(4-chloro...

In the methanol solvate of the title 1:1 cocrystal, C(29)H(28)F(6)N(4)OS·C(5)H(9)NO(2)·CH(4)O, the l-proline mol-ecule exists as a zwitterion. In the crystal, the disubstituted thio-urea, l-proline and methanol mol-ecules are linked by N-H⋯O and N-H⋯N hydrogen bonds, forming a two-dimensional array in the ab plane.

the 2-mono and 2,6-disubstituted methyl-1,4-dihydropyridines were synthesized by reaction of morpholine, thiophenol, 8-hydroxyquinoline, 2-naphthol and 2-mercopto-1-methyl imidazole with the 2-mono bromo and 2,6-dibromo-1,4-dihidropyridines.