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Paper | Special issue | Vol 56, No. 1-2, 2002, pp.123-128
Published online, 1st January, 1970
DOI: 10.3987/COM-00-S(K)4
Practical Synthesis of Both Enantiomers of Vasopressin V2 Receptor Antagonist OPC-41061 Using the Catalytic Asymmetric Hydrogenation

Hiroshi Yamashita,* Tadaaki Ohtani, Seiji Morita, Kenji Otsubo, Keizo Kan, Jun Matsubara, Kazuyoshi Kitano, Yoshikazu Kawano, Minoru Uchida, and Fujio Tabusa

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


The optically active enantiomers of 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061, 1) were enantioselectively synthesized. The asymmetric transfer hydrogenation of the ketone (2), which is the precursor of 1, gave the corresponding secondary alcohols in good yield and excellent enantiomeric excess.