1996-29-8, These common heterocyclic compound, 1996-29-8, name is 1-Bromo-4-chloro-2-fluorobenzene, 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.
1-bromo-4-chloro-2-fluorobenzene (5g, 23.9 mmol, 1 eq), 2-methylpiperazine (2.8 g, 1.15 eq), tris – dipalladium (O) (0.43g, 0,05 equiv), rac-BINAP (0.89g, 0.15 eq), sodium tert- butoxide (3.2 g, 1.4 eq) was slurried in toluene (60 mL), followed by the mixture was heated overnight at 65 C.. After cooling to room temperature, it was added ethyl acetate (100mL). The black precipitate was removed by filtration. The filtrate was washed twice with 3N potassium carbonate solution. The organic phase was dried over sodium sulfate, the solid was neutralized with 2N HCl-ether was collected by filtration, washed with ether, and dried in vacuo 1- (4-chloro-2-fluorophenyl) -3- It was obtained methyl piperazine as the dihydrochloride salt.
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 1996-29-8.
Reference:
Patent; CHEMOCENTRYX INCORPORATED; ZHANG, PENGLIE; ZENG, YIBIN; (41 pag.)JP5654467; (2015); B2;,
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