Chen, Xiu-Ping published the artcileStudy on the mild, rapid and selective difluorocarbene-mediated triclassification of iododifluoroacetophenone with secondary amines and tree model for product classification, Recommanded Product: 4-Methoxy-N-methylaniline, the main research area is difluoromethyl benzoimidazole preparation; indole difluoromethyl preparation; formamide aryl preparation; benzothiazole difluoromethyl thio preparation; benzooxazole difluoromethyl thio preparation; aryl difluoromethoxy preparation.
In this work, a room temperature difluorocarbene-mediated triclassification reaction of iododifluoroacetophenone and secondary amines with mild condition, short reaction time (only 10 min) and high selectivity had been studied, which produced one of the following three substances: N-CF2H derivatives I [R1 = H, SCF2H, 2-pyridyl, (3,4-dichlorophenyl)methyl; R2 = H, CN, C(O)Me, (2-chloropyrimidin-4-yl); R3 = H, 5-Br, 6-NO2, 5,6-di-Me, 6-Me-5-NO2; X = C, N; Y = C, N] (up to 87% yield), formamides ArNR4C(O)H [Ar = Ph, 4-MeOC6H4, 1-naphthyl; R4 = Me, Et] (82-89% yield) or the recycled starting secondary amines. This phenomenon was related to the structural stability of the corresponding products. If unstable, it would be hydrolyzed to formamides first, and then further hydrolyzed to starting amines. Based on the geometric structure of the raw materials, the corresponding prediction tree model was established, which provided guidance for the further application of difluoromethylation of Vemurafenib and AZD9291. In addition, this method was successfully applied to the S- and O-difluoromethylations to obtain the corresponding sulfur derivatives II [Z = S, O; R5 = 5-Cl, 6-Br, 4-Me, etc.] and O-CF2H derivatives ArO-CF2H [Ar = 3,4-di-MeOC6H3 1-naphthyl, 4-PhC6H4, etc.] with satisfactory yields.
Tetrahedron published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 5961-59-1 belongs to class isoquinoline, name is 4-Methoxy-N-methylaniline, and the molecular formula is C8H11NO, Recommanded Product: 4-Methoxy-N-methylaniline.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem