Preparation And Analysis Of Optical M-nisoldipine Enantiomers

Among the various drugs currently available for the treatment of systematic hypertension, the calcium channel antagonists continue to receive much attention as a result of their benefits in the prevention of cardiovascular events and other complication. m-nisoldipine, as a new dihydropyridine calcium ion antagonist, was firstly composed in school of pharmacy, Hebei Medical University. It is stable in the form of solid when exposed to light, while nisoldipine lost activity under lighting condition for 30min.Objective: Optically active 1, 4-dihydro-2, 6-dimethyl-4-(3-nitrophnyl)-3, 5-Pyridinedicarboxylate methyl 2-methylpropyl esters [(S)-(+)-m-nisoldipine and (R)-(-)-m-nisoldipine] were synthesized with high optical purities from (R)-(-)- and (S)-(+)- 1, 4-dihydro-5-methoxycarbonyl-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylic acid [(S)-(+)-monomethyl ester and (R)-(-)- monomethyl ester], which are available from (±)-monomethyl ester by optical resolution using cinchonidine and quinidine, respectively. A simple and rapid high performance liquid chromatographic method has been developed for the direct resolution of (±)-monomethyl ester and m-nisoldipine...