Application of 849937-96-8, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 849937-96-8 as follows.
To a solution of 5-bromo-2,4-dichloropyridine (CAS 849937-96-8) (22.95 g, 96.1 mmol, Eq: 1.00) in Toluene (352 mL) and Water (48.0 mL) was added Pd(OAc)2 (431 mg, 1.92 mmol, Eq: 0.02), butyldi-l-adamantylphosphine (1.03 g, 2.88 mmol, Eq: 0.03), potassium cyclopropyltrifluoroborate (CAS 1065010-87-8) (14.9 g, 101 mmol, Eq: 1.05) and Cs2C03 (62.6 g, 192 mmol, Eq: 2.0). The resulting reaction mixture was stirred at 110C overnight and controlled by TLC. The reaction was found to be only partially complete so 0.5 more equivalents (7.5 g) of potassium cyclopropyltrifluororate were added (3 times). Reaction mixture concentrated in vacuo then diluted with ethyl acetate and the solution poured into a separatory funnel. Extraction with aqueous saturated NaHC03, organic phase dried over NaS04 and evaporated down to dryness. Flash chromatography with a 330 g Si02 column, eluent mixture of heptane and ethyl acetate giving 7.39 g of the desired product (Yield 40%). MS (ESI, m/z): 188.2 (M).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,849937-96-8, its application will become more common.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; GAVELLE, Olivier; GRETHER, Uwe; KIMBARA, Atsushi; NETTEKOVEN, Matthias; ROEVER, Stephan; ROGERS-EVANS, Mark; ROMBACH, Didier; SCHULZ-GASCH, Tanja; WO2014/154612; (2014); A1;,
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