Some common heterocyclic compound, 15205-11-5, name is 2-Chloro-4-fluorobenzylamine, molecular formula is C7H7ClFN, 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. Formula: C7H7ClFN
3-Methyl-5-(2-methylpropyl)-1 /-/-pyrazol-4-yl]acetic acid (0.170 g, 0.43 mmol, prepared as described below) was dissolved in a mixture of dimethylformamide (1 ml) and dichloromethane (3 ml) and and to this was added water soluble carbodiimide (0.099 g, 0.52 mmol), 1-hydroxybenzotriazole (0.070 g, 0.52 mmol), and N-ethyl morpholine (0.164 ml, 1.29 mmol). The mixture was stirred for 10 minutes and then [(2-chloro-4-fluorophenyl)methyl]amine (0.082 g, 0.52 mmol) was added. The mixture was stirred overnight at room temperature and then saturated aqueous sodium hydrogen carbonate (2 ml) was added to the mixture. After stirring for a further 10 minutes the organic phase was separated by filtration through a hydrophobic frit. The aqueous layer was washed with a further aliquot of dichloromethane (2-3 ml) and the organic phase was again separated and then the combined organic phases were evaporated to give the crude product as a yellow oil. The crude material was purified by mass-directed automated HPLC to give the pure product as a white solid after freeze-drying of the collected product fractions (0.080 g)-LC/MS [M+H]+ = 338 retention time = 2.32 minutes.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 15205-11-5, its application will become more common.
Reference:
Patent; GLAXO GROUP LIMITED; WO2007/141267; (2007); A1;,
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