Electric Literature of 1940-29-0, A common heterocyclic compound, 1940-29-0, name is 4-Bromo-3,5-dichloroaniline, molecular formula is C6H4BrCl2N, 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.
A microwave vial containing 4-bromo-3,5-dichloroaniline (350 mg, 1.45 mmol, Eq: 1.00), 2- methoxypyridin-4-ylboronic acid (289 mg, 1.89 mmol, Eq: 1.3), sodium carbonate (394 mg, 3.72 mmol, Eq: 2.56) and bis(triphenylphosphine)palladium (II) chloride (65 mg, 92.6 flmol, Eq:0.0637) was degassed with Argon for 15 min. DME (8 mL) and water (2 mL) was added and the reaction was heated for 30 min with the microwave at 115 deg. The reaction mixture was concentrated, diluted with ethyl acetate, washed with brine, dried with sodium sulfate and chromatographed (40g Redisep, 100% to 10% ethyl acetate/hexane) to give 254 mg (65%) of desired product as a colorless oil.
The synthetic route of 1940-29-0 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BERTHEL, Steven Joseph; CHEN, Zhi; CHI, Feng; CHIN, Elbert; ERICKSON, Shawn David; GABRIEL, Stephen Deems; KOCER, Buelent; Mertz, Eric; PLANCHER, Jean-Marc; WEIKERT, Robert James; WO2014/135471; (2014); A1;,
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