Electric Literature of 117324-05-7,Some common heterocyclic compound, 117324-05-7, name is Ethyl 2-amino-4-fluorobenzoate, molecular formula is C9H10FNO2, 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.
A total of 3.84 g of 2-amino-4-fluoro-benzoic acid ethyl ester obtained in Production Example II-7-a was dissolved in 50 ml of pyridine, 1.64 ml of acetyl chloride was added under ice-cooling, and the mixture was stirred for 1 hours. The reaction mixture was diluted with water and was extracted with diethyl ether. The resulting organic layer was washed with 1 N hydrochloric acid and brine, dried over magnesium sulfate, and then evaporated, to give 4.0 g of the title compound.1H-NMR ( 400 MHz, CDCl3 ) d 1.41 ( 3H, t, J = 6.8 Hz ), 2.14 ( 3H, s ), 4.38 ( 2H, q, J = 6.8 Hz ), 6.73 – 6.81 ( 1H, m ), 8.06 ( 1H, dd, J = 8.8, 6.4 Hz ), 8.53 ( 1H, dd, J = 12.0, 2.4 Hz ), 11.3 ( 1H, brs )
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Ethyl 2-amino-4-fluorobenzoate, its application will become more common.
Reference:
Patent; Eisai Co., Ltd.; EP1380576; (2004); A1;,
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