Some tips on 1003-98-1

Statistics shows that 2-Bromo-4-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 1003-98-1.

Synthetic Route of 1003-98-1, These common heterocyclic compound, 1003-98-1, name is 2-Bromo-4-fluoroaniline, 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 148:; 148 EPO To a N, N-dimethyl-formamide solution (10 mL) of ethyl (3R)-3-[(tert-butoxycarbonyl)amino]hex-5- ynoate (1.26 g, 4.94 mmol) was added 4-fluoro-2-iodoaniline (1.29 g, 5.44 mmol), diisopropylamine (15 mL), dichlorobis(triphenylphosphine)-palladium (II) (76 mg, 0.109 mmol) and CuI (31 mg, 0.163 mmol). The mixture was stirred at 25C for 15h after three circles of nitrogen/vacuum flush. DMF was removed by vacuum and the residue was diluted with EtOAc (75 mL). It was then washed with NH4CI solution (1×50 mL) and brine (2×50 mL), dried with Na2SO4 and concentrated. After column chromatography (12% ethyl acetate in hexane), the title compound was obtained in 88% yield (1.58g). 1H NMR (CDCI3): delta 6.95 (1 H, m), 6.84 (1 H, m), 6.64 (1 H, m), 5.26 (1 H, br s), 4.22-4.10 (3H, m), 2.82-2.60 (4H, m), 1.44 (9H, s), 1.27 (3H, t, J=7.1 Hz).

Statistics shows that 2-Bromo-4-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 1003-98-1.

Reference:
Patent; PFIZER, INC.; WO2006/40646; (2006); A1;,
Bromide – Wikipedia,
bromide – Wiktionary