1354792-75-8Relevant academic research and scientific papers
Decarboxylative and Deaminative Alkylation of Difluoroenoxysilanes via Photoredox Catalysis: A General Method for Site-Selective Synthesis of Difluoroalkylated Alkanes
Song, Heng,Cheng, Ran,Min, Qiao-Qiao,Zhang, Xingang
supporting information, p. 7747 - 7751 (2020/10/09)
A general method for site-selective difluoroalkylation of alkyl carboxylic redox esters with difluoroenoxysilanes through photoredox-catalyzed decarboxylative reaction has been developed. The reaction can also be extended to aliphatic amine derived pyridinium salts. This method has the advantages of high efficiency, mild reaction conditions, and broad substrate scope, including primary, secondary, and sterically hindered tertiaryl alkyl substrates, providing a general and practical route for applications in organic synthesis and pharmaceutical studies.
Copper-Catalyzed Deaminative Difluoromethylation
Cai, Aijie,Liu, Wei,Wang, Yufei,Yan, Wenhao,Yang, Dongqi,Yang, Kundi,Zacate, Samson B.,Zeng, Xiaojun
supporting information, p. 16398 - 16403 (2020/07/17)
The difluoromethyl group (CF2H) is considered to be a lipophilic and metabolically stable bioisostere of an amino (NH2) group. Therefore, methods that can rapidly convert an NH2 group into a CF2H group would be of great value to medicinal chemistry. We report herein an efficient Cu-catalyzed approach for the conversion of alkyl pyridinium salts, which can be readily synthesized from the corresponding alkyl amines, to their alkyl difluoromethane analogues. This method tolerates a broad range of functional groups and can be applied to the late-stage modification of complex amino-containing pharmaceuticals.
Copper-Catalyzed Decarboxylative Difluoromethylation
Zeng, Xiaojun,Yan, Wenhao,Zacate, Samson B.,Chao, Tzu-Hsuan,Sun, Xiaodong,Cao, Zhi,Bradford, Kate G. E.,Paeth, Matthew,Tyndall, Sam B.,Yang, Kundi,Kuo, Tung-Chun,Cheng, Mu-Jeng,Liu, Wei
supporting information, p. 11398 - 11403 (2019/08/20)
We report herein a highly efficient Cu-catalyzed protocol for the conversion of aliphatic carboxylic acids to the corresponding difluoromethylated analogues. This robust, operationally simple and scalable protocol tolerates a variety of functional groups and can convert a diverse array of acid-containing complex molecules to the alkyl-CF2H products. Mechanistic studies support the involvement of alkyl radicals.
(3-(4-(AMINOMETHYL)PHENOXY OR PHENYLTHIO)AZETIDIN-1-YL)(5-PHENYL-1,3,4-OXADIAZOL-2-YL)METHANONE COMPOUNDS
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Page/Page column 46, (2012/01/15)
Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
