Chemistry:Monatepil
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Monatepil is a calcium channel blocker and α1-adrenergic receptor antagonist used as an antihypertensive.[1]
Synthesis
The synthesis of monatepil was first disclosed in patents filed by Dainippon Pharmaceutical.[2]
- upright=2
The amino group of the dihydrodibenzothiepin (1) is first reacted with the acid chloride of 4-chlorobutyric acid, to give the amide (3). This is then used to alkylate para-fluorophenylpiperazine (4) to yield monatepil.[2][3]
References
- ↑ "Relative contribution of alpha 1-adrenoceptor blocking activity to the hypotensive effect of the novel calcium antagonist monatepil". Journal of Cardiovascular Pharmacology 26 (1): 55–60. July 1995. doi:10.1097/00005344-199507000-00009. PMID 7564365.
- ↑ 2.0 2.1 Hitoshi Uno, et al., "Calcium antagonist piperazine derivatives, and compositions therefor", US patent 4749703, issued 1988-06-07, assigned to Dainippon Pharmaceutical Co Ltd
- ↑ Kurokawa, Mikio; Sato, Fuminori; Fujiwara, Iwao et al. (1991). "A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11-dihydrodibenzo[b,e]thiepin maleate and related compounds". Journal of Medicinal Chemistry 34 (3): 927–934. doi:10.1021/jm00107a009. PMID 2002473.
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