Synthetic Route of 847729-27-5, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.847729-27-5, name is Methyl 2-chloro-5-fluoronicotinate, molecular formula is C7H5ClFNO2, molecular weight is 189.57, as common compound, the synthetic route is as follows.
STEP 2. Methyl 5-fluoro-2- (4-fluorobenzvl) nicotinate; To a stirred solution of methyl 2-chloro-5-fluoronicotinate (step 1, 350 mg, 1.85 mmol) and dichlorobis [triphenylphosphine] nickel (1I) (362 mg, 0.55 mmol) in tetrahydrofuran (15 mL) was added a 0.5 M solution of 4-fluorobenzylzinc chloride in tetrahydrofuran (5.54 mL, 2.77 mmol) at 0 C under nitrogen. The resulting mixture was warmed to room temperature and stirred for 16 h. The mixture was poured into saturated aqueous ammonium chloride solution (50 mL) and extracted with ethyl acetate (100 ML). The organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was purified by flush column chromatography on silica gel eluting with hexane/ethyl acetate (10/1) to afford 439 mg (90%) of the title compounds as colorless oil: H-NMR (CDC13) 6 8.56 (1H, d, J = 2.8 Hz), 7.91 (1H, dd, J = 8.6, 2.9 Hz), 7.26-7. 19 (2H, m), 6.98-6. 92 (2H, M), 4.52 (2H, s), 3.89 (3H, s); MS (ESI) m/z 264 (M + H) +.
Statistics shows that 847729-27-5 is playing an increasingly important role. we look forward to future research findings about Methyl 2-chloro-5-fluoronicotinate.
Reference:
Patent; PFIZER INC.; PFIZER JAPAN, INC.; WO2005/21508; (2005); A1;,
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