Monatepil Explained

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]

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]

Notes and References

  1. Sugimoto T, Hosoki K, Karasawa T . 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 . 7564365 . 10.1097/00005344-199507000-00009. 1548014 . free .
  2. US . 4749703 . Hitoshi Uno, et al. . Calcium antagonist piperazine derivatives, and compositions therefor . patent . 1988-06-07 . 1985-08-09 . Dainippon Pharmaceutical Co Ltd.
  3. 10.1021/jm00107a009 . 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 . 1991 . Kurokawa . Mikio . Sato . Fuminori . Fujiwara . Iwao . Hatano . Naonobu . Honda . Yayoi . Yoshida . Takayuki . Naruto . Shunsuke . Mastumoto . Junichi . Uno . Hitoshi . 3 . Journal of Medicinal Chemistry . 34 . 3 . 927–934 . 2002473 .

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