Novel Synthesis of Arylethynyl Heterocycles

Novel Synthesis of Arylethynyl-Heterocyles

The tosyl group has been one of the most commonly used groups to protect, activate and chelate indoles for lithiation at position 2. In the course of one of our synthetic programs, 1-tosyl-2-(pmethoxyphenylacetyl)indole (1a) was prepared in excellent yields starting from N-tosylindole by 2lithiation, transformation of the resulting 2-lithio derivative into the 2-trimethylstannylindole derivativ...

synthesis of novel phosphorus heterocycles as antimicrobial agents

Synthesis and antimicrobial activity of some novel heterocycles containing thiazole, oxazole, thiazine, oxazine and triazole moiety

Indandione 1 was brominated to yield 2-bromoIndandione 2 which on further reacted with substituted thiocarbamides, carbamides, 2-aminothiophenols, 2-aminophenol and triazoles to furnished 3-substituted aniline-2-thia-4-aza-6,7-benzo-8-oxo-bicyclo [3.3.0]-1(5),3-octadiene 3, 3-substituted aniline-2-oxa-4-aza-6,7-benzo-8-oxo-bicyclo [3.3.0]-1(5),3-octadiene 4, 2-Thia-5-aza-9-oxo-3,4-(3’-substitut...

Design and synthesis of novel D-ring fused steroidal heterocycles.

Using dehydroepiandrosterone as the starting material, we have synthesized a series of steroid analogs possessing a D-ring fused with heterocycles which are pyridine, imidazo [2,1-b]thiazoles or substituted thiazole imines. All the final structures are first reported and identified by NMR and MS spectroscopys, the yields of these products are moderate to good and the reaction conditions are mil...

Synthesis of saturated N-heterocycles.

Saturated N-heterocycles are prevalent in biologically active molecules and are increasingly attractive scaffolds in the development of new pharmaceuticals. Unlike their aromatic counterparts, there are limited strategies for facile construction of substituted saturated N-heterocycles by convergent, predictable methods. In this Synopsis, we discuss recent advances in the synthesis of these comp...