On December 31, 1998, Kawanishi, Hiroyuki; Morimoto, Hiroshi; Nakano, Takao; Watanabe, Tatsuya; Oda, Kuniyuki; Tsujihara, Kenji published an article.Category: chlorides-buliding-blocks The title of the article was Stereoselective synthesis of antifungal sulfoximines, novel triazoles II. And the article contained the following:
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. The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Category: chlorides-buliding-blocks
The Article related to triazole sulfoximine derivative preparation, sulfoximine triazole prospective antifungal agent nonracemic stereoselective practical preparation, stereoselective synthesis antifungal sulfoximine novel triazole, antifungal activity triazole sulfoximine nitrogen substitution, chlorophenylethanesulfonic acid tcpes novel resolving agent sulfoximine triazole and other aspects.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics