New downstream synthetic route of Methyl 4-bromo-3-(trifluoromethyl)benzoate

107317-58-8, name is Methyl 4-bromo-3-(trifluoromethyl)benzoate, belongs to esters-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: esters-buliding-blocks

107317-58-8, name is Methyl 4-bromo-3-(trifluoromethyl)benzoate, belongs to esters-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: esters-buliding-blocks

General procedure: A suspension of 4-(((lS,4S,5R)-2-azabicyclo[2.2.1]heptan-5-yoxy)methy)-5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazole hydroiodide salt l2dd (0.52 mrnol, 1 equiv.),methyl4-bromo-2/3-substituted benzoate 106-y (0 68 mmol, 1.3 equiv.), Cs2C03 (1.3 mmol,15 2.5 equiv.), Pd?(dha)3 (0.15 equiv.), BINAP (0.2 equiv.) in Toluene (10.0 mL) was heatedunder a nitrogen atmosphere at 1 J 0C for 16 h. The reaction rnixture was cooled to roomtemperature, diluted with ethyl acetate and filtered through a pad ofCelite. The organic layerwas washed with brine, dried over anhydrous Na2S04, filtered and concentrated 1..mderreduced pressure. The crude material v.·as purified on ISCO silica gel column20 chromatography using hexane/ethyl acetate as eluents to give the desired methyl ester l06zwhich was used as such in the next step.

The synthetic route of 107317-58-8 has been constantly updated, and we look forward to future research findings.

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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