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1: Bioorg Med Chem Lett. 2005 Feb 15;15(4):1055-9.Click here to read Links

Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.

Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y.

Pharmaceutical Research and Technology Center, Dainippon Pharmaceutical Co., Ltd, 5-51, Ebie 1-chome, Fukushima-ku, Osaka 553-0001, Japan. takeshi-ochi@dainippon-pharm.co.jp

Two major metabolites in humans of blonanserin, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta-[b]pyridine (code name AD-5423), were synthesized. The first, 7-hydroxylated AD-5423, was synthesized through a four-step process starting from 4-fluorobenzoylacetonitrile (1), and the second, 8-hydroxylated AD-5423, a nine-step process also from 1. The optical resolution, structures, and receptor binding properties of the metabolites were documented.

PMID: 15686911 [PubMed - indexed for MEDLINE]