SYNTHESIS OF THE PIPERIDINONE METABOLITES OF PIPERIDINE TYPE PHENOTHIAZINE ANTIPSYCHOTIC-DRUGS VIA RUTHENIUM TETROXIDE OXIDATION

被引:46
作者
LIN, G
MIDHA, KK
HAWES, EM
机构
[1] College of Pharmacy, University of Saskatchewan, Saskatoon, Saskatchewan
关键词
D O I
10.1002/jhet.5570280202
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The lactam metabolites of the piperidine type phenothiazine antipsychotic drugs thioridazine, mesoridazine and sulforidazine were synthesized in six steps from commercially available 2-(2-hydroxyethyl)piperidine. The key step involved ruthenium tetroxide oxidation of N-protected 2-(2-chloroethyl)piperidine. The products were then oxidized to obtain the phenothiazine ring 5-sulfoxide analogues.
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页码:215 / 219
页数:5
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