These common heterocyclic compound, 63069-50-1, name is 4-Amino-3-fluorobenzonitrile, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. SDS of cas: 63069-50-1
General procedure: 1.4.1. MethodAlj00243j A mixture of the amino aromatic or heteroaromatic starting material (1 eq), Ag2SO4 (1 eq) and 12 (1 eq) in EtOH is stirred at temperatures ranging from room temperature to 50C for a period which can vary from 1 h to approximately 16 h. The mixture is filtered, concentrated and diluted in an organic solvent. The organic mixture undergoes aqueous work up. The solvent is removed under reduced pressure and the residue is purified by flash column chromatography to yield the desired product.1.4.2. Illustrative example ofmethodAl: synthesis of 4-Amino-3-fluoro-5-iodo-benzonitrile (Int.4).N NH2 NI H2j00244j A mixture of 4-amino-3-fluorobenzonitrile (147 mmol), 12 (147 mmol) and Ag2SO4 (147 mmol) in EtOH (700 mL) was stirred at room temperature for 1.5 h. The mixture was filtered and concentrated. The residue was dissolved in EtOAc and washed (sat. Na2S2O3 x 3). The organic layer was dried (Na2SO4) and concentrated. The residue was purified by flash column chromatography (Si02, 95:5 to 70:3 0 cyclohexane/EtOAc) to yield the desired product.
The synthetic route of 4-Amino-3-fluorobenzonitrile has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GALAPAGOS NV; MENET, Christel, Jeanne, Marie; MAMMOLITI, Oscar; BLANC, Javier; OR?ULIC, Mislav; RO?CIC, Maja; WO2015/110378; (2015); A1;,
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