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A facile synthetic route to the new thiazol-5-ylboronic acid pinacol ester was described herein. Its reactivity toward Suzuki cross-coupling reaction was studied to provide various 5-arylthiazoles. A comparative study between Suzuki cross-coupling reactions and palladium-catalyzed C5–H direct arylation on thiazole ring was achieved. Graphical abstract Full-size image (11K)

This paper sets forth a global synthetic strategy based on the Garlanding concept to design and to produce halo-oligopyridines. This strategy allows to prepare an infinite number of these new compounds and hence to create a library of halo-oligopyridines. This article is focused on the basic principle of the Garlanding concept and on the demonstration of its feasibility. Graphical abstract

The synthesis and the biological evaluation of pyrano[3,2-e]indoles and their reaction intermediates are described. The compounds prepared were evaluated for their inhibition of NO production, antioxidant activity and also for their ability to inhibit in vitro the growth of four human tumor cell lines: large lung carcinoma (COR-L23), alveolar basal epithelial carcinoma (A549), amelanotic melanoma (C32) and melanoma (A375). The two reaction intermediates, 5a and 5b, showed the highest inhibition of NO production in murine monocytic macrophage (IC50=1.1μM and IC50=2.3 μM respectively). Compound 5a was the most active against melanotic melanoma (IC50=11.8μM) while the other compounds exhibited weak cytotoxicity with IC50 values >50μM on all cell lines.

2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile was converted into the corresponding 2-(pyrrol-1-yl) derivative, followed by reduction of the latter compound into the corresponding amine. This amine and its acyl, aroyl, and arylidene derivatives were used as synthons in the synthesis of several title compounds

[Normal View 5K | Magnified View 12K] The reaction between 3-(dimethylamino)/3,3-bis(methylthio)-1-(substituted)prop-2-en-1-ones and 4-substituted-5-amino-1H-pyrazoles afforded new pyrazole[1,5-a]pyrimidines structurally related to Zaleplon. The chemical modifications introduced at the 3-, 5-, and 7-positions of the bicyclic structure revealed new promising candidates for the treatment of sleep disorders.

The syntheses of the title heterocycles were achieved using 5-amino-1-(1-benzyl-1H-indol-3-ylcarbonyl)-1H-pyrazole-4-carbonitrile as starting material. These compounds were converted into the 4-imidazolinyl derivatives which were subjected to cyclization reactions to afford the title compounds.