39562-17-9Relevant articles and documents
Preparation method of benidipine hydrochloride
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Paragraph 0048-0051, (2021/04/21)
The invention belongs to the field of chemical synthesis of drugs, and particularly relates to a preparation method of a hypotensive drug benidipine hydrochloride. The method comprises the following steps: carrying out a Knoevenagel reaction, a Michael addition reaction, cyclization and hydrolysis on starting raw materials 3-nitrobenzaldehyde and methyl acetoacetate in the presence of a catalyst, reacting with thionyl chloride, directly reacting with 1-benzyl-3-hydroxypiperidine, and refining to obtain the benidipine hydrochloride. The benidipine hydrochloride obtained by adopting the preparation method of the benidipine hydrochloride is high in purity, column chromatography isolation is not needed, and the HPLC purity of the product is 99.5% or above. The yield of the obtained benidipine hydrochloride is relatively high and can reach 68% or above.
An expedient synthesis of β-acetamido- and β-benzamidocarbonyl compounds via KAL(SO4)2·12H2O-catalyzed three-component coupling reaction
Molla, Aniruddha,Hussain, Sahid
, p. 494 - 503 (2013/12/04)
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Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of nitrendipine analogues
Zhou, Kai,Wang, Xiao-Meng,Zhao, Yi-Zhi,Cao, Yong-Xiao,Fu, Qiang,Zhang, San-Qi
scheme or table, p. 1325 - 1330 (2012/06/04)
The antihypertensive activity of nitrendipine analogues can be improved by properly lengthening its alkyl chain in 3- or 5-position. Nitrendipine and its seven analogues were synthesized, and their antihypertensive activities in spontaneously hypertensive rats (SHR) were evaluated by ig administration. It was found that 5-n-heptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4- dihydropyridine- 3,5-dicarboxylate [(±)-5] exhibited the strongest antihypertensive effect amongst eight compounds. (?)-5-nheptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine- 3,5-dicarboxylate [(+)-5] was also prepared. Antihypertensive activities of (±)-5 and (?)-5 in SHR were compared. The results showed that (±)-5 and (?)-5 had a higher potency than nitrendipine, and (+)-isomer was 1.79-fold the raceme at a dose of 2 mg/kg. Springer Science+Business Media, LLC 2010.