Shi, Hang; Braun, Augustin; Wang, Lu; Liang, Steven H.; Vasdev, Neil; Ritter, Tobias published the artcile< Synthesis of 18F-Difluoromethylarenes from Aryl (Pseudo) Halides>, Recommanded Product: tert-Butyl (4-bromophenyl)(methyl)carbamate, the main research area is fluoromethyl arene 18F labeled chemoselective preparation; fluoroacetophenone chemoselective preparation bromination fluorination deacylation; coupling aryl halide pseudohalide fluoroacetophenone bromination substitution fluoride deacylation; bromination substitution 18F fluoride deacylation arylfluoromethyl phenyl ketone; aryl (pseudo) halides; difluoromethylarenes; fluorine-18; positron emission tomography; radiopharmaceuticals.
A general, operationally simple, and chemoselective method for the synthesis of [18F]difluoromethylarenes such as I (R = 18FFCH) from [18F]fluoride and aryl chlorides, bromides, iodides, and triflates or pseudohalides such as I (R = TfO) is reported. Coupling of the aryl halides or pseudohalides to α-fluoroacetophenone in the presence of a palladium biphenylamine precatalyst yields α-fluoro-α-arylmethyl Ph ketones such as I (R = PhCOCHF); α-bromination and substitution with [18F]fluoride, tetraethylammonium bromide, and N-bromophthalimide in acetonitrile and chlorobenzene followed by deacylation with aqueous KOH yielded mono-[18F]-labeled difluoromethylarenes such as I (R = 18FFCH) in 10-60% radiochem. yields. The method was used to prepared 18F-difluoromethylated analogs of pharmaceuticals such as Claritin, fluoxetine (Prozac), and DAA1106.
Angewandte Chemie, International Edition published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 639520-70-0 belongs to class bromides-buliding-blocks, and the molecular formula is C12H16BrNO2, Recommanded Product: tert-Butyl (4-bromophenyl)(methyl)carbamate.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary