期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 4, 页码 1055-1059出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.12.028
关键词
blonanserin; AD-5423; hydroxyl metabolites; antipsychotic agent
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. (C) 2004 Elsevier Ltd. All rights reserved.
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