Reference of 1256834-13-5 , The common heterocyclic compound, 1256834-13-5, name is 4-Bromo-6-chloronicotinic acid, molecular formula is C6H3BrClNO2, 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.
To a solution of 6-bromo-4-chloronicotinic acid (3 g, 12.69 mmol) in DMF (42 mL) was added HATU (6.27 g, 16.49 mmol), (R)-4-amino-3-fluoro-2-methylbutan-2-ol hydrochloride (2.4 g, 15.23 mmol), and N,N-Diisopropylethylamine (5.62 ml, 32.26 mmol). The resulting solution was stirred at room temperature overnight and subsequently diluted with ethyl acetate. The organic solution was washed with saturated aqueous lithium chloride (3 times), then dried over Na^SCri. and then concentrated. The residue was purified by silica gel chromatography (eluent: EtO Ac/hexanes) to provide (R)-6-bromo-4-chloro-N-(2-fluoro-3-hydroxy-3- methylbutyl)nicotinamide.ES/MS: 341.1 (M+H+).
The synthetic route of 1256834-13-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GILEAD SCIENCES, INC.; AMMANN, Stephen; BACON, Elizabeth M.; BRIZGYS, Gediminas; CHIN, Elbert; CHOU, Chienhung; COTTELL, Jeromy J.; NDUKWE, Marilyn; TAYLOR, James G.; WRIGHT, Nathan E.; YANG, Zheng-Yu; ZIPFEL, Sheila M.; (138 pag.)WO2020/36979; (2020); A1;,
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