Electric Literature of 15205-11-5,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.
Tert-butyl 2,4-dichloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-6-car boxylate (8.30 g, 27.2 mmol) prepared according to Process Step 1 was dissolved in tetrahydrofuran (80 mL), and the solution was mixed with 2-chloro-4-fluorobenzylamine (8.69 g, 54.4 mmol) and triethylamine (11.4 mL), followed by stirring at 40 C for 15.5 hours. Crystals precipitated in the reaction mixture were separated by filtration, and the solvent was distilled off from the filtrate. The precipitated crystals were reslurried from a 3:1 mixture of hexane and ethyl acetate and thereby yielded tert-butyl 2-chloro-4-(2-chloro-4-fluorobenzylamino)-5,6,7,8-tetrahydro pyrido [4,3-d]pyrimidine-6-carboxylate (9.99 g, 23.4 mmol, in a yield of 86%).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Chloro-4-fluorobenzylamine, its application will become more common.
Reference:
Patent; KYOWA HAKKO KOGYO CO., LTD.; EP1552842; (2005); A1;,
Chloride – Wikipedia,
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