These common heterocyclic compound, 93919-56-3, name is (4-(Trifluoromethoxy)phenyl)methanamine, 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. COA of Formula: C8H8F3NO
A mixture of 2- (5-amino-2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yl) -2-phenylacetic acid (50 mg, 0.13 mmol) , (4- (trifluoromethoxy) phenyl) methanamine (29 mg, 0.15 mmol) , HATU (55 mg, 0.15 mmol) and DIPEA (50 mg, 0.39 mmol) in DMF (10 mL) was stirred for 4 hours at RT. The reaction mixture was poured into H 2O (20 mL) and extracted with EtOAc (50 mL x 3) . The combined organic layers were washed with brine, dried over Na 2SO 4, concentrated and purified by column chromatography (petroleum ether/EtOAc =1: 1100%EtOAc) to give target compound (39.3 mg, 55.2%) . 1H NMR (400 MHz, DMSO-d6) delta 8.55 (s, 1H) , 8.24 (s, 1H) , 8.20 (br. s, 2H) , 7.95 (s, 1H) , 7.47 -7.27 (m, 9H) , 7.24 (d, J = 3.2 Hz, 1H) , 6.74 (br. s, 1H) , 6.48 (s, 1H) , 4.45 -4.27 (m, 2H) ppm. MS: M/e 549 (M+1) +.
The synthetic route of (4-(Trifluoromethoxy)phenyl)methanamine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BEIGENE, LTD.; ZHANG, Guoliang; ZHOU, Changyou; (152 pag.)WO2019/196803; (2019); A1;,
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