- TRIAZOLYLPIPERIDINE DERIVATIVES AND USE THEREOF IN THERAPY
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The present invention provides compounds of formula (I) Wherein R1 , R2, R3 , R4 , Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.
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Page/Page column 35
(2010/11/25)
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- SYNTHESIS OF OXOSULFONIUM SALTS BY THE OXIDATION OF SULFONIUM SALTS
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A general synthetic method for oxosulfonium salts by oxidation of sulfonium salts with sodium perbenzoate (or sodium m-chloroperbenzoate) was developed.In case of the oxidation of aryldimethylsulfonium salts, the corresponding oxosulfonium salts (1e-h) were obtained in 64-91percent yields.Diphenylmethylsulfonium and triphenylsulfonium salts were also oxidized with sodium perbenzoate to afford the corresponding oxosulfonium salts (1i and 1j) in 75 and 58percent yields, respectively.Trialkylsulfonium salts such as trimethylsulfonium, dimethyloctylsulfonium, S-methylthiolanium, and S-methyl(pentamethylene)sulfonium salts, were also oxidized to the corresponding oxosulfonium salts (1a-d) in good yields.To clarify the reaction mechanisms, the oxidation of bicycloheptane-1-sulfonium salt (5) was investigated and found to afford oxosulfonium salt (6) in 50percent yield.A reaction mechanism involving nucleophilic attack by perbenzoate anion on the cationic sulfur atom of sulfonium salt and giving an S-O sulfurane intermediate is proposed.
- Mori, Mitsuo,Takeuchi, Hiroyuki,Minato, Hiroshi,Kobayashi, Michio,Yoshida, Masato,et al.
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p. 157 - 164
(2007/10/02)
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