- BENIDIPINE HYDROCHLORIDE
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Disclosed is a method for preparing benidipine hydrochloride, which comprising: 1) during the pre-treatment stage including acylchloridizing the main ring of dihydropyridine and then linking the side chain to synthesize directly benidipine hydrochloride, ultrasound technology is introduced, and the reactant material is dispersed and dissolved by untrasound to increase reaction rate; and/or 2) during the post-treatment stage, ultrasound technology is introduced and crude crystals or product obtained by heating to dryness of benidipine hydrochloride obtained via the method described above or any other synthetic routes is dissolved once more and then highly purified benidipine hydrochloride is obtained by untrasound.
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Page/Page column 5; 6
(2012/11/07)
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- Synthesis and pharmacological activity of stereoisomers of 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 1-(phenylmethyl)-3-piperidinyl ester
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1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 1-(phenylmethyl)-3-piperidinyl ester 1, a highly potent calcium antagonist, was separated into stereo- and optical isomers to investigate the differences of antihypertensive activities between them. Fractional crystallization of the hydrochlorides of 1 gave α- and β-diasterioisomers. The α-isomer (benidipine hydrochloride, KW-3049) showed very strong hypotensive effect, but little activity was observed in the β-isomer. From optically resolved 1,4-dihydro-5-methoxycarbonyl-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridi necarboxylic acids 2, and 1-benzyl-3-piperidinols 3, four optical isomers of 1 were synthesized, and their absolute configurations were deduced. The hypotensive activity of (+)-α, namely (S)-(S)-1, was 30 to 100 times stronger than that of (-)-α in intravenously administered spontaneously hypertensive rats.
- Muto,Kuroda,Kawato,Karasawa,Kubo,Nakamizo
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p. 1662 - 1665
(2007/10/02)
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