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Communication | Special issue | Vol 50, No. 1, 1999, pp.17-20
Published online, 1st January, 1970
DOI: 10.3987/COM-98-S(H)6
An Efficient Synthesis of a Metabolite of Vasopressin V2 Receptor Antagonist, OPC-31260, by Metalloporphyrin-catalyzed Demethylation

Yoshikazu Kawano, Kenji Otsubo,* Jun Matsubara, Kazuyoshi Kitano, Tadaaki Ohtani, Seiji Morita, and Minoru Uchida

*Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Kagasuno 463-10, Kawauchi-cho, Tokushima 771-0192, Japan


A secondary amine (3) as a metabolite of the vasopressin V2 receptor antagonist, OPC-31260 (1), was efficiently prepared through selective demethylation of the corresponding N,N-dimethylalkylamine N-oxide (2) with meso-(tetraphenylporphinato)iron(III) chloride [Fe( TPP)]Cl, where tetrazole as an additive played a crucial role in the achievement of high chemical yields.