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2005
Pyrazine derivatives
R 0550
Syntheses and Properties of the Major Hydroxy Metabolites in Humans of
AD-5423, a Novel Antipsychotic Agent. — The synthesis of the
25- 157 Blonanserin
two major metabolites, the 7-hydroxylated AD-5423 (VIII) and the 8-hydroxylated
AD-5423, are achieved in four- and nine-step procedures from fluorobenzoylacetonitrile (I), respectively. Chiral resolution of (VIII) yields the corresponding optically pure
alcohols. An in vitro metabolism study reveals (S)-(VIII) as a main metabolite, whose
absolute configuration is determined by X-Ray crystallography. All stereoisomers
show lower affinities to the human D2L and 5HT2A receptors than the parent AD-5423.
Isomers having (R)-configuration display a higher affinity to the receptors than their
respective isomers. — (OCHI*, T.; SAKAMOTO, M.; MINAMIDA, A.; SUZUKI, K.;
UEDA, T.; UNE, T.; TODA, H.; MATSUMOTO, K.; TERAUCHI, Y.; Bioorg. Med.
Chem. Lett. 15 (2005) 4, 1055-1059; Pharm. Res. Technol. Cent., Dainippon Pharm.
Co., Ltd., Fukushima, Osaka 553, Japan; Eng.) — H. Hoennerscheid
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