Synthetic Route of 15205-11-5, A common heterocyclic compound, 15205-11-5, name is 2-Chloro-4-fluorobenzylamine, molecular formula is C7H7ClFN, 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.
Example 281-[(2-Chloro-4-fluorophenyl)methyl]-4-(4-fluoro-2,6-dimethylphenyl)-2,3- piperazinedione (E28)Methyl [(4-fluoro-2,6-dimethylphenyl)(2-oxoethyl)amino](oxo)acetate (0.15 g, 0.49 mmol) was dissolved in dichloromethane (5 ml) and cooled to O0C. 4 Angstrom molecular seives (0.3 g, 0.49 mmol), acetic acid (0.09 ml, 1.48 mmol), 2-chloro-4- fluorobenzylamine (0.07 ml, 0.54 mmol) and sodium triacetoxyborohydride (0.16 g, 0.74 mmol) were added. After 5 minutes, the reaction was warmed to room temperature and stirred for 16 hours overnight. Saturated aqueous sodium bicarbonate (5 ml) was added and the mixture stirred for 10 minutes. The organic layer was separated using a hydrophobic frit and concentrated in vacuo. The crude material was purified by mass-directed automated HPLC to yield 1-[(2-chloro-4- fluorophenyl)methyl]-4-(4-fluoro-2,6-dimethylphenyl)-2,3-piperazinedione (0.083 g) as a white solid. LC/MS [M+H]+ = 379, retention time = 2.84 minutes.
The synthetic route of 15205-11-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXO GROUP LIMITED; CHAMBERS, Laura Jane; DEAN, David Kenneth; MUNOZ-MURIEDAS, Jorge; STEADMAN, Jon Graham Anthony; WALTER, Daryl Simon; WO2010/125103; (2010); A1;,
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