Role of Hetero-halogen (F · · · X, X = Cl, Br, and I) or homo-halogen (X · · · X, X = F, Cl, Br, and I) interactions in substituted benzanilides
A series of halogen-substituted benzanilides have been synthesized and characterized, and crystallization studies directed toward generation of polymorphs have been performed to delineate the importance of interactions involving halogens. The effect of ha
Nayak, Susanta K.,Kishore Reddy,Row, Tayur N. Guru,Chopra, Deepak
experimental part
p. 1578 - 1596
(2012/04/04)
Synthesis of pharmacologically relevant indoles with amine side chains via tandem hydroformylation/fischer indole synthesis
The sequence of hydroformylation and Fischer indole synthesis starting from amino olefins and aryl hydrazines is described. In a convergent manner, the two units bearing pharmacologically relevant substituents are assembled in the final indolization step. This modular and diversity-oriented approach to tryptamines and homotryptamines can be conducted in water and allows synthesis of branched and nonbranched tryptamines as well as tryptamine-based pharmaceuticals such as the 5-HT1D agonist L 775 606.