- Synthesis of expected metabolites of benidipine hydrochloride
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(±)-(R*)-2,6-Dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5- dicarboxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049, 1) a highly potent and long-acting calcium antagonistic 1,4-dihydropyridine derivative, is now under clinical study as an antihypertensive and as an antianginal agent. In order to confirm the structures of the metabolites of KW-3049, 19 compounds were prepared. Among then 11 compounds were found to be metabolites (the compounds 2, 3, 6, 8, 14, 15, 16, 28, 31, 32 and 34) of KW-3049 in rats and/or dogs.
- Muto,Kuroda,Kawato,Nishikawa,Nakamizo
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p. 1666 - 1670
(2007/10/02)
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- 1,4-Dihydropyridine derivatives
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New 1,4-dihydropyridine derivatives of the formula [I] are provided: STR1 wherein R1 represents a C1-4 alkyl group or a C3-6 alkoxyalkyl group, R2 represents a C1-8 alkyl group, and A represents an unsubstituted hexamethylene group or a substituted hexamethylene group having one or two C1-3 alkyl groups. The 1,4-dihydropyridine derivatives have vasodilating and hypotensive activity which is kept for a long period, and are useful in the treatment of cardiovascular disease and hypertention.
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