Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent |
| |
| Authors: | Ochi Takeshi Sakamoto Masato Minamida Akira Suzuki Kenji Ueda Tomohiko Une Teruaki Toda Hiroshi Matsumoto Kazuya Terauchi Yoshiaki |
| |
| Affiliation: | 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 |
| |
| Abstract: | 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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
