53012-84-3Relevant articles and documents
LPAR1 Inhibitor. Medical application and preparation method thereof
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Paragraph 0072-0074; 0081-0082, (2021/10/05)
LPAR1 Inhibitor, medical application and preparation method thereof, and the structural general formula I of the inhibitor is as follows. In-flight RX Alkyl groups selected from H, C1 - C6, COOCH3 , CF3 , NO2 ,
Indium-Catalyzed C?F Bond Transformation through Oxymetalation/β-Fluorine Elimination to Access Fluorinated Isocoumarins
Yata, Tetsuji,Nishimoto, Yoshihiro,Chiba, Kouji,Yasuda, Makoto
supporting information, p. 8288 - 8294 (2021/05/21)
Fluorinated heterocycles have attracted much attention in the pharmaceutical and agrochemical industries. Many strategies have already been developed to achieve the synthesis of fluorinated heterocycles. Formidable challenges remain, however, in the synthesis of fluorinated isocoumarin derivatives that are among the most alluring structural motifs. Herein, the indium-catalyzed C?F bond transformation of 2-(2,2-difluorovinyl) benzoates is reported, which are readily accessible compounds, to give a diverse array of fluorinated isocoumarins. The present reaction proceeds smoothly using inexpensive reagents: a catalytic amount of indium salt in the presence of zinc salt. A theoretical calculation of potential energy profiles showed that the reaction consists of oxymetalation with the elimination of alkyl halide and the β-fluorine elimination.
Electrophilic Aromatic Formylation with Difluoro(phenylsulfanyl) methane
Betterley, Nolan M.,Kongsriprapan, Sopanat,Chaturonrutsamee, Suppisak,Deelertpaiboon, Pramchai,Surawatanawong, Panida,Pohmakotr, Manat,Soorukram, Darunee,Reutrakul, Vichai,Kuhakarn, Chutima
, p. 2033 - 2040 (2018/03/21)
Difluoro(phenylsulfanyl)methane (PhSCF 2 H) was found to undergo a reaction with aromatic compounds mediated by SnCl 4, through a thionium intermediate characterized by NMR and TD-DFT analyses, leading to the formation of a mixture of S, S ′-diphenyl dithioacetal and aromatic aldehyde which, after oxidative hydrolysis, provides the aromatic aldehyde in good to excellent yields. The salient feature of the present work is the reaction of activated aromatic compounds containing a deactivating ester functional group, leading to the formylated products in good yields.
