Synthetic Route of 59247-47-1, 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 59247-47-1 as follows.
To a 250 mL round-bottom flask ‘.vas added (lS,4R,5R)-5-[[5-cyclopropyl-3-(2-cyclopropyl-6-fluoropheny)-1,2-oxazol-4-y l]methoxy ]-2-azabicyclo[2.2.1]heptan-3-one10 3lle (300 mg, 0.78 mmol, 1.00 equiv.), Pd1(dba)3 (36 mg, 0.04 mmoL 0.05 equiv.),XantPhos (46 mg, 0.08 mmol, 0.10 equiv.), Cs£03 (384 mg, 1.18 mmol, 1.50 equiv.), tol (5mL), and tert-hutyl 4-bromobenzoate (301 mg, 1.17 mmol, 1.50 equiv.). The resultingmixture vvas heated at ll0°C ovemight ·with stirring. After cooling to room temperature, themixture vvas diluted with 50 mL ofH20, extracted with ethyl acetate (100 mL x 2), and the15 combined organic extracts were washed with brine (100 mL x 2), dried, and concentrated.The residue was purified by silica gel column chromatography eluting with ethylacetate/hexane (2: l) to give tert-butyl 4-[(l S,4R,SR)-5-[[ 5-cyclopropyl-3-(2-cyclopropyl-6-fluorophenyl)-1,2-oxazol-4-yl]methoxy ]-3-oxo-2-azabicyclo[2.2.1 ]heptan-2-yl]benzoate 311 f(300 mg, 68percent) as a yellow oil.
According to the analysis of related databases, 59247-47-1, the application of this compound in the production field has become more and more popular.
Reference:
Patent; ARDELYX, INC.; CHAO, Jianhua; JAIN, Rakesh; HU, Lily; LEWIS, Jason Gustaf; BARIBAULT, Helene; CALDWELL, Jeremy; (582 pag.)WO2018/39386; (2018); A1;,
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