446-63-9Relevant articles and documents
SUBSTITUTED TRICYCLIC COMPOUNDS
-
Page/Page column 120, (2021/06/04)
Disclosed are compounds of the general formula (I), its tautomeric form, its stereoisomer, its pharmaceutically acceptable salt, its polymorph, or solvate thereof, Formula (I) wherein, ring A, R1 to R5, X, Y, m, and n are as defined herein, for use as SOS1 inhibitors in the treatment of proliferative, infectious and RASopathy diseases or disorders. Also disclosed are methods of synthesizing the compound of formula I, pharmaceutical compositions containing the compound of formula I, method of treatment of proliferative, infectious and RASopathy diseases or disorder, for example, a cancer, by administering the said compound and combinations of the compound of formula I with other active ingredients.
Palladium-Catalyzed Suzuki–Miyaura Cross-Coupling of Secondary α-(Trifluoromethyl)benzyl Tosylates
Brambilla, Marta,Tredwell, Matthew
supporting information, p. 11981 - 11985 (2017/09/20)
A palladium-catalyzed C(sp3)?C(sp2) Suzuki–Miyaura cross-coupling of aryl boronic acids and α-(trifluoromethyl)benzyl tosylates is reported. A readily available, air-stable palladium catalyst was employed to access a wide range of functionalized 1,1-diaryl-2,2,2-trifluoroethanes. Enantioenriched α-(trifluoromethyl)benzyl tosylates were found to undergo cross-coupling to give the corresponding enantioenriched cross-coupled products with an overall inversion in configuration. The crucial role of the CF3 group in promoting this transformation is demonstrated by comparison with non-fluorinated derivatives.
Enzymatic resolution by CALB of organofluorine compounds under conventional condition and microwave irradiation
Ribeiro, Sandra S.,Raminelli, Cristiano,Porto, André L.M.
, p. 53 - 59 (2013/11/06)
Enzymatic kinetic resolution of organofluorine rac-alcohols by CALB yielded ( )-(R)-2,2,2-trifluoro-1- phenylethanol (2a), ()-(R)-1-(3-bromophenyl)-2,2,2- trifluoroethanol (2b), ()-(R)-1-(4-bromophenyl)- 2,2,2-trifluoroethanol (2c), ()-(S)-1-(2,4,5-trifluorophenyl)ethanol (2d), (+)-(S)-2,2,2-trifluoro-1- phenylethyl acetate (3a), (+)-(S)-1-(3-bromophenyl)-2,2,2-trifluoroethyl acetate (3b), (+)-(S)-1-(4- bromophenyl)-2,2,2-trifluoroethyl acetate (3c) and (+)-(R)-1-(2,4,5-trifluorophenyl)ethyl acetate (3d) in high enantiomeric excess (up to >99% ee). The reactions were conducted under conventional conditions (orbital shaking) and microwave irradiation in toluene and vinyl acetate as acylating agent. The CALB showed excellent selectivities and good yields in the transesterification of fluorinated aromatic compounds.