Synthetic studies on medicinally important compounds

Abstract

Compounds of 4-Aryl-1,4-dihydropyridine (DHP) type are the most effective calcium channel blockers, which are widely used in the treatment of hypertension and coronary heart diseases. Among them, felodipine, amlodipine, and nitrendipine, exist as a mixture of enantiomers and one of the two isomers is more effective in their pharmacological effects. With this point of view, we have carried out the studies on synthesis of enantioselective dihydropyridine compounds by using (R)-glycidol as a starting compound for the chiral auxiliary and selective transesterification as a key reaction. Thus, we have successfully developed a novel synthetic route to dihydropyridine analogs that can be applied to industrial process. Also, we studied JAK-3 inhibitors for immunosuppression. Recently, the development of a novel JAK3 inhibitor named CP-690,550 was reported. This compound has high efficacy for the prevention of allograft rejection. Our synthetic studies were focused on the efficient synthesis of CP-690,550. In addition to CP-690,550, we also designed and synthesized compounds based on CP-690,550.