Kawanishi, Hiroyuki published the artcileStereoselective synthesis of antifungal sulfoximines, novel triazoles II, Safety of trimethyloxosulphonium chloride, the publication is Heterocycles (1998), 181-190, database is CAplus.
Novel triazole derivatives I (R = H, MeCO, MeNHCO, Me, MeO2CCH2) with an N-substituted sulfoximine moiety were synthesized and evaluated for antifungal activity. These compounds showed significantly weaker activity than I (R = H); the N-H moiety of the sulfoximine was extremely important for the activity. A practical and effective stereoselective synthesis of (-)-I (R = H), considered to be the most promising antifungal compound, has been developed. (-)-I (R = H) is prepared in seven steps, including two resolution steps, from the methylthiodifluoropropiophenone II, by epoxidation with Me3SO+ Cl–, diastereoselective sulfimine formation with chloramine T, addition of 1,2,4-triazole to the epoxide, oxidation of the sulfimine, acid hydrolysis of toluenesulfonyl group of the sulfoximine, and resolution with the novel resolving agent 1-(2,3,4-trichlorophenyl)ethanesulfonic acid [(+)-TCPES] III.
Heterocycles published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Safety of trimethyloxosulphonium chloride.
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