Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 1210838-82-6, name is 5-Bromo-3-ethynylpyridin-2-ylamine. A new synthetic method of this compound is introduced below., Product Details of 1210838-82-6
Step 3: 5-Bromo-3-(3-(((tert-butyldimethylsilyl)oxy)methyl)isoxazol-5-yl)pyridin-2-amine To a suspension of 5-bromo-3-ethynylpyridin-2-amine (Intermediate C15) (500 mg, 2.54 mmol) and sodium ascorbate (0.254 ml, 0.254 mmol) in t-BuOH (10 ml) and water (10ml) under N2 was added copper(ll) sulfate pentahydrate (13mg, 0.051 mmol, 2mol%) and NaHCOs (853mg, 10.15mmol) followed by 2-((tert-butyldimethylsilyl)oxy)-N- hydroxyacetimidoyl chloride (step 3) (1.7g, 7.61 mmol, 3eq) slowly over 15mins. The mixture was stirred at RT overnight. The resulting mixture was extracted into DCM, washed with water, brine, the organic layer separated, dried over MgS04, filtered and the solvent removed under reduced pressure. The crude product was purified by flash column chromatography elution with iso-hexane:ethyl acetate (0-30%) on a 24g silica cartridge. The required fractions were combined and the solvent removed under reduced pressure to afford the title compound; LCMS: Rt = 1.62mins MS m/z 384.4 [M+H]+; Method 2minl_owpHv03.
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Reference:
Patent; NOVARTIS AG; BELLENIE, Benjamin Richard; BLOOMFIELD, Graham Charles; BRUCE, Ian; CULSHAW, Andrew James; HALL, Edward Charles; HOLLINGWORTH, Gregory; NEEF, James; SPENDIFF, Matthew; WATSON, Simon James; WO2015/162456; (2015); A1;,
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