Reference of 112734-22-2,Some common heterocyclic compound, 112734-22-2, name is (4-Bromo-2-fluorophenyl)methanamine, molecular formula is C7H7BrFN, 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.
N-[(4-Bromo-2-fluorophenyl)methyl]-4-tert-butylbenzamide In a 25-mL round bottom flask purged and maintained with an inert atmosphere of nitrogen, (4-bromo-2-fluorophenyl)methanamine (1.000 g, 4.90 mmol, 1.00 equiv) was dissolved in dichloromethane (20 mL), to which were added 4-tert-butylbenzoic acid (1.310 g, 7.35 mmol, 1.50 equiv), HOBT (993 mg, 7.35 mmol, 1.50 equiv), EDCI (1.409 g, 7.35 mmol, 1.50 equiv) and DIEA (1.267 g, 9.80 mmol, 2.00 equiv) in sequence at room temperature. The resulting solution was stirred for 16 h at room temperature. When the reaction was done, it was quenched by the addition of 10 mL water and the mixture was extracted with ethyl acetate (3*20 mL). The organic layers were combined, dried over sodium sulfate and concentrated under reduced pressure. The residue was purified in a silica gel column eluting with ethyl acetate in petroleum ether (5% to 30% gradient) to afford N-[(4-bromo-2-fluorophenyl)methyl]-4-tert-butylbenzamide (700 mg, 39%) as yellow solid.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route (4-Bromo-2-fluorophenyl)methanamine, its application will become more common.
Reference:
Patent; Merck Patent GmbH; GAILLARD, Pascale; SEENISAMY, Jeyaprakashnarayanan; LIU-BUJALSKI, Lesley; CALDWELL, Richard D.; POTNICK, Justin; QIU, Hui; NEAGU, Constantin; JONES, Reinaldo; WON, Annie Cho; GOUTOPOULOS, Andreas; SHERER, Brian A.; JOHNSON, Theresa L.; GARDBERG, Anna; (234 pag.)US2016/96834; (2016); A1;,
Bromide – Wikipedia,
bromide – Wiktionary