54251-80-8Relevant academic research and scientific papers
PROCESS OF MAKING CFTR MODULATORS
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Paragraph 0418-0420; 0756; 0757, (2021/02/19)
The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
Synthesis of γ-Keto Sulfones through a Three-Component Reaction of Cyclopropanols, DABCO ? (SO2)2 and Alkyl Halides
Zhang, Chun,Zhang, Chao,Tang, Jie,Ye, Shengqing,Ma, Mingliang,Wu, Jie
supporting information, p. 3109 - 3114 (2021/05/03)
A route to γ-keto sulfones through a metal-free reaction of cyclopropanols, DABCO ? (SO2)2 and alkyl halides is described. This reaction occurs under mild conditions in the absence of any catalysts, additives, or oxidants. Various functional groups including as ester, amino, methoxy, bromo, trifluoromethyl, nitro and carbonyl are tolerated well in this transformation, and the corresponding γ-keto sulfones are afforded in 35% to 95% yields. The proposed mechanism implies that this reaction proceeds through γ-keto sulfinate intermediate generated in situ, which further undergoes nucleophilic substitution with alkyl halides leading to γ-keto sulfones. (Figure presented.).
Iron-Catalyzed Triazole-Enabled C-H Activation with Bicyclopropylidenes
Mo, Jiayu,Messinis, Antonis M.,Oliveira, Joa? C. A.,Demeshko, Serhiy,Meyer, Franc,Ackermann, Lutz
, p. 1053 - 1064 (2021/01/26)
C-H/C-C functionalizations with oxymethylated bicyclopropylidenes were accomplished with an iron catalyst under external oxidant-free conditions. The combination of the unique reactivity of bicyclopropylidenes with a robust iron(II) catalyst enabled C-C c
Rh-Catalyzed cascade C-H activation/C-C cleavage/cyclization of carboxylic acids with cyclopropanols
Wang, Siqi,Miao, Erfei,Wang, Hao,Song, Bichao,Huang, Wei,Yang, Weibo
supporting information, p. 5929 - 5932 (2021/06/18)
Merging both C-H and C-C activation in a tandem process is a marked challenge. A novel Rh(iii)-catalyzed C-H activation/ring opening C-C cleavage/cyclization of carboxylic acids with cyclopropanols was developed for the synthesis of 3-substituted phthalides andα,β-butenolides. This reaction displays excellent functional group tolerance with respect to both carboxylic acids and cyclopropanols and features relatively mild conditions. Remarkably, the utility of this method was highlighted by the rapid construction of bioactive compounds bearing a 3-substituted phthalide frameworkvialate-stage functionalization.
Copper-mediated tandem ring-opening/cyclization reactions of cyclopropanols with aryldiazonium salts: Synthesis of: N -arylpyrazoles
Liu, Jidan,Xu, Erjie,Jiang, Jinyuan,Huang, Zeng,Zheng, Liyao,Liu, Zhao-Qing
supporting information, p. 2202 - 2205 (2020/02/26)
A general method for the synthesis of structurally diverse N-arylpyrazoles from readily available cyclopropanols and aryldiazonium salts is disclosed. The reaction was conducted at room temperature within minutes with a broad substrate scope and excellent regioselectivity.
Ni-Catalyzed Denitrogenative Cross-Coupling of Benzotriazinones and Cyclopropanols: An Easy Access to Functionalized β-Aryl Ketones
Li, Jincan,Zheng, Yan,Huang, Mingxian,Li, Wanfang
supporting information, p. 5020 - 5024 (2020/07/03)
A novel Ni-catalyzed denitrogenative cross-coupling between benzotriazinones and cyclopropanols is reported herein. This neoteric reactivity allows for the convenient synthesis of β-(o-amido)aryl ketones from readily available starting materials with good yields (up to 93percent) and general substrate scope.
MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR
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Page/Page column 285; 286, (2018/06/30)
Compounds of Formula (I) pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.
NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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Page/Page column 194, (2009/01/20)
The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
