Highly polar potential metabolites of the neuroleptic agent oxyprothepin: Synthesis of 2-hydroxy-8-methylsulfonyl and 3-hydroxy-8-methylsulfonyl derivatives of 10-[4-( …
J Jílek, J Holubek, E Svátek, J Schlanger…
文献索引:Jilek; Holubek; Svatek; et al. Collection of Czechoslovak Chemical Communications, 1985 , vol. 50, # 2 p. 519 - 537
Abstract The acid XI, obtained by reaction of (2-iodo-5-methoxyphenyl) acetic acid with 4- (methylsulfonyl) thiophenol (VIII) in dimethylformamide in the presence of potassium carbonate and copper, was transformed via intermediates XIIa-XIVa to compound XVa. Demethylation with boron tribromide afforded compound III, the potential metabolite of oxyprothepin (II). Its oxidation with hydrogen peroxide in acetic acid gave the sulfoxide ...