1520-31-6Relevant academic research and scientific papers
One-Pot Synthesis of N-Iodo Sulfoximines from Sulfides
Zupanc, An?e,Jereb, Marjan
, p. 5991 - 6000 (2021/05/05)
This is the first report on the synthesis and characterization of N-iodo sulfoximines. The synthesis was designed as a room temperature one-pot cascade reaction from readily available sulfides as starting compounds, converted into sulfoximines by reaction with ammonium carbonate and (diacetoxyiodo)benzene, followed by iodination with N-iodosuccinimide or iodine in situ, in up to 90% isolated yields, also at a multigram scale. Iodination of aryls with N-iodo sulfoximines, oxidation, and conversion to N-SCF3 congeners have been demonstrated.
Nickel-Catalyzed N-Arylation of NH-Sulfoximines with Aryl Halides via Paired Electrolysis
Liu, Dong,Liu, Zhao-Ran,Ma, Cong,Jiao, Ke-Jin,Sun, Bing,Wei, Lei,Lefranc, Julien,Herbert, Simon,Mei, Tian-Sheng
supporting information, p. 9444 - 9449 (2021/03/29)
A novel strategy for the N-arylation of NH-sulfoximines has been developed by merging nickel catalysis and electrochemistry (in an undivided cell), thereby providing a practical method for the construction of sulfoximine derivatives. Paired electrolysis is employed in this protocol, so a sacrificial anode is not required. Owing to the mild reaction conditions, excellent functional group tolerance and yield are achieved. A preliminary mechanistic study indicates that the anodic oxidation of a NiII species is crucial to promote the reductive elimination of a C?N bond from the resulting NiIII species at room temperature.
BIARYL DERIVATIVE, PREPARATION METHOD THEREOF AND PHARMACEUTICAL APPLICATION THEREOF
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Paragraph 0099; 0140; 0141, (2020/12/22)
Disclosed are a biaryl derivative having a structure represented by Formula (I) and inhibitory activity against PD-1/PD-L1 interaction, a preparation method thereof, and a pharmaceutical application thereof. The series of compounds of the present inventio
HETEROCYCLIC INHIBITORS OF ATR KINASE
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, (2019/09/30)
The present disclosure relates to heterocyclic compounds and methods which inhibit ATR kinase to treat or prevent cancer.
I2/PhI(OAc)2 Copromoted Amination Reaction: Synthesis of α-Dicarbonylsulfoximine Derivatives by Incorporating an Intact Dimethyl Sulfoxide
Zhao, Peng,Wu, Xia,Geng, Xiao,Wang, Can,Zhou, You,Wu, Yan-Dong,Wu, An-Xin
supporting information, p. 8322 - 8329 (2019/06/27)
An I2/PhI(OAc)2 copromoted strategy using dimethyl sulfoxide as an "S/C2/O" source for preparing α-dicarbonylsulfoximine derivatives is reported. This process involves oxidative coupling to construct a C-N bond and electrophilic amin
HETEROCYCLIC INHIBITORS OF ATR KINASE
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Paragraph 0656; 0660-0661, (2019/02/01)
The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
PYRROLO[2,3-C]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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Page/Page column 50, (2018/08/03)
Disclosed are a pyrrolo[2,3-c]pyridine derivative, a preparation method therefor, and use thereof in medicine. Specifically, disclosed are a pyrrolo[2,3-c]pyridine derivative as represented by general formula (1), a preparation method therefor, a pharmaceutical composition comprising the derivative, as well as use thereof as a BRD4 inhibitor in the treatment of related diseases such as cancers, inflammations, chronic liver diseases, diabetes, cardiovascular diseases and AIDS, each substituent in general formula (I) being same as defined in the description.
SULFOXIMINE, SULFONIMIDAMIDE, SULFONDIIMINE AND DIIMIDOSULFONAMIDE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2, 3-DIOXYGENASE
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Paragraph 210-211, (2018/06/12)
Provided are certain IDO inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
Copper-catalyzed oxidative decarboxylative coupling of α-keto acids and sulfoximines
Pimpasri, Chaleena,Sumunnee, Ladawan,Yotphan, Sirilata
supporting information, p. 4320 - 4327 (2017/07/10)
A copper-catalyzed oxidative decarboxylative coupling of α-keto acids with NH-sulfoximines has been developed. With CuBr as the catalyst and K2S2O8 as the oxidant, this reaction enables the formation of a C-N bond and gives N-aroylsulfoximine products in moderate to excellent yields. The reaction mechanism is likely to involve the generation of a reactive aroyl radical intermediate.
Metal-Free, Phosphonium Salt-Mediated Sulfoximination of Azine N-Oxides: Approach for the Synthesis of N-Azine Sulfoximines
Aithagani, Sravan Kumar,Kumar, Mukesh,Yadav, Mahipal,Vishwakarma, Ram A.,Singh, Parvinder Pal
, p. 5886 - 5894 (2016/07/23)
Herein, we report a simple and metal-free method for the synthesis of N-azine sulfoximines by the nucleophilic substitution of azine N-oxides with NH-sulfoximines. The present method works at room temperature with wide functional group compatibility and gives several unprecedented N-azine sulfoximines. The reaction conditions were also found suitable with enantiopure substrates and furnished products without any racemization. It also finds an application in the sulfoximination of azine-based functional molecules such as 2,2′-bipyridine, 1,10-phenanthroline, and quinine.
