121034-18-2Relevant academic research and scientific papers
Sulfoxide-to-sulfilimine conversions: Use of modified Burgess-type reagents
Hendriks, Christine M. M.,Lamers, Philip,Engel, Julien,Bolm, Carsten
, p. 3363 - 3368 (2013)
Sulfoxides can directly be converted into N-cyanosulfilimines using a new Burgess-type reagent. By applying this strategy with a related reagent variant, synthetically valuable NH-sulfoximines have been prepared from sulfoxides via N-protected sulfilimines. The practical three-step reaction sequence is generally high yielding and applicable to a wide range of substrates. The sulfoxide-to-sulfilimine conversion can also be performed under solvent-reduced conditions in a ball mill. Copyright
Rhodium(iii)-catalyzed cascade C-H functionalization/annulation of sulfoximines with iodonium ylides for the synthesis of cyclohexanone-1,2-benzothiazines
Chen, Lu,Hao, Liqiang,Ji, Yafei,Wang, Yangyang,Wang, Zhichao,Wu, Gaorong,Xu, Xiaobo
supporting information, p. 887 - 894 (2022/02/03)
A highly efficient Rh(iii)-catalyzed cascade C-H activation/annulation of sulfoximines with iodonium ylides under metal-oxidant-free conditions has been reported. The fused cyclohexanone-1,2-benzothiazine scaffold is readily achieved with a one-pot proces
Efficient Kinetic Resolution of Sulfur-Stereogenic Sulfoximines by Exploiting CpXRhIII-Catalyzed C?H Functionalization
Brauns, Marcus,Cramer, Nicolai
supporting information, p. 8902 - 8906 (2019/06/04)
Chiral sulfoximines with stereogenic sulfur atoms are promising motifs in drug discovery. We report an efficient method to access chiral sulfoximines through a C?H functionalization based kinetic resolution. A rhodium(III) complex equipped with a chiral Cpx ligand selectively participates in conjunction with phthaloyl phenylalanine in the C?H activation of just one of the two sulfoximine enantiomers. The intermediate reacts with various diazo compounds, providing access to chiral 1,2-benzothiazines with synthetically valuable substitution patterns. Both sulfoximines and 1,2-benzothiazines were obtained in high yields and excellent enantioselectivity, with s-values of up to 200. The utility of the method is illustrated by the synthesis of the key intermediates of two pharmacologically relevant kinase inhibitors.
Rhodium(III)-Catalyzed C?H Alkynylation of N-Methylsulfoximines
Wang, Tao,Wang, Yi-Ning,Wang, Rui,Wang, Xi-Sheng
supporting information, p. 2449 - 2452 (2018/08/17)
A rhodium(III)-catalyzed direct C?H alkynylation of a wide range of N-methylsulfoximines with (bromoethynyl)triisopropylsilane has been developed. This protocol is compatible with both (S,S)-diaryl sulfoximines and (S,S)-alkyl aryl sulfoximines, and shows mild conditions, and good functional group tolerance. The synthetic utility of this method has been demonstrated by subsequent various transformations of the products.
FUSED PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 65, (2017/05/07)
A series of substituted pyrazolo[1,5-a]pyrimidine and pyrazolo[1,5-a][1,3,5]- triazine derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase ΙΙΙβ (ΡI4ΚΙΙΙβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
Rhodium-catalyzed direct synthesis of unprotected NH-sulfoximines from sulfoxides
Miao, Jinmin,Richards, Nigel G. J.,Ge, Haibo
supporting information, p. 9687 - 9689 (2014/08/18)
A novel rhodium-catalyzed imination of sulfoxides using O-(2,4-dinitrophenyl)hydroxylamine is developed under mild conditions with good functional group tolerance. This method provides an efficient access to free NH-sulfoximines, an important structural u
SULPHOXIMINE-SUBSTITUTED QUINAZOLINE DERIVATIVES AS IMMUNO-MODULATORS, THEIR PREPARATION AND USE AS MEDICAMENTS
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Page/Page column 12-13, (2009/07/25)
The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.
NOVEL SULPHOXIMINE-SUBSTITUTED QUINAZOLINE AND QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 35, (2009/01/20)
The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) f
Optical Resolution of Sulfoximines by Complex Formation with Optically Active 2,2'-Dihydroxy-1,1'-binaphthyl or 1,6-Di(o-chlorophenyl)-1,6-diphenylhexa-2,4-diyne-1,6-diol
Mori, Koji,Toda, Fumio
, p. 1997 - 2000 (2007/10/02)
Some alkyl aryl and dialkyl sulfoximines were resolved efficiently by complex formation with optically active 2,2'-dihydroxy-1,1'-binaphthyl and 1,6-di(o-chlorophenyl)-1,6-diphenylhexa-2,4-diyne-1,6-diol, respectively.
