Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 15205-11-5, name is 2-Chloro-4-fluorobenzylamine, A new synthetic method of this compound is introduced below., Quality Control of 2-Chloro-4-fluorobenzylamine
Example 221-[(2-Chloro-4-fluorophenyl)methyl]-4-(2,6-dimethylphenyl)-2,3-piperazinedione(E22)Methyl [(2,6-dimethylphenyl)(2-oxoethyl)amino](oxo)acetate (0.27 g, 1.0 mmol) and 2-chloro-4-fluorobenzylamine (0.19 g, 1.2 mmol) were stirred in 2% acetic acid/methanol (10 ml) for 5 minutes, whereupon polymer-supported cyanoborohydride (0.98 g, 4.0 mmol) was added. The mixture was stirred at room temperature for 16 hours. The resin was filtered off using an SCX cartridge (Varian, 5g), washing through with methanol. The filtrate was concentrated in vacuo to afford the crude product as a gum. The crude material was purified twice by flash-silica gel chromatography (first eluting with a 0-25% gradient of methanol in dichloromethane; then re-purified using a 0-100% gradient of ethyl acetate in iso-hexane) to afford 1- [(2-chloro-4-fluorophenyl)methyl]-4-(2,6-dimethylphenyl)-2,3-piperazinedione (0.11 g)-LC/MS [M+H]+ = 361 , retention time = 2.78 minutes.
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
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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