Application background and overview of 2-bromo-5-hydroxypyridine
2-Bromo-5-hydroxypyridine boronic acid can be used as a pharmaceutical and chemical synthesis intermediate. If 2-bromo-5-hydroxypyridine is inhaled, move the patient to fresh air; if there is skin contact, take off contaminated clothing, rinse the skin thoroughly with soap and water, and seek medical attention if you feel uncomfortable; if the eyes are clear, In case of contact, separate eyelids, rinse with running water or saline, and seek medical attention immediately; if ingested, rinse mouth immediately, do not induce vomiting, and seek medical attention immediately.
Applications of 2-bromo-5-hydroxypyridine
2-Bromo-5-hydroxypyridine can be used as a pharmaceutical and chemical synthesis intermediate. If the following reaction can occur:
2-Bromo-5-hydroxypyridine (200 mg, 1.15 mmol) and tetrakis(triphenylphosphine)palladium(0) (66 mg, 0.06 mmol) were suspended in DME (5 mL). After 10 minutes, SM-1 (410 mg, 1.26 mmol) and 2N Na2CO3 aqueous solution (1.7 mL) were added. The reaction was then purged twice with argon and heated to 100°C in a microwave reactor for 20 minutes. After cooling, the reaction mixture was diluted with EtOAc, washed with water and brine, dried over NaSO, filtered and concentrated. The resulting residue was purified on SiO2 (EtOAc/heptane) to afford intermediate 95-B.
In addition, 2-bromo-5-hydroxypyridine can also undergo the following reactions:
Combine 2-bromo-5-hydroxypyridine (4.00g, 23mmol) and 4-((methylsulfonyloxy)methyl)piperidine-1-carboxylic acid tert-butyl ester (7.08g, 24mmol) A solution of N-methylpyrrolidone (50 mL) was treated with Cs2CO3 (9.74 g, 30 mmol). and heated to 100°C overnight. The reaction mixture was then diluted with ethyl acetate, extracted 3 times with water, dried with MgSO4, filtered, evaporated and crystallized with toluene/hexane to give B2b; (M-ΔBu+H)+C12H16BrN2O3 ESIMS m/z calculated: 315.0, found: 315.0.
