Reference of 69812-51-7, These common heterocyclic compound, 69812-51-7, name is Methyl 4-chlorosulfonylbenzoate, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
6-[3-(2,6-dichloro-phenyl)-5-isopropyl-isoxazol-4-ylmethoxy]-2-trifluoromethyl-pyridin-3-ylamine from example 5, step 4 (0.132g, 0.30mmol) was dissolved in dry acetonitrile (5ml) followed by the addition of 4-chlorosulfonyl-benzoic acid methyl ester (0.070g, 0.33mmol) and pyridine (0.071g, 0.90mmol). The reaction mixture was stirred for 12h at 50C, N-methylmorpholine (0.03g, 0.3mmol) was added and stirring was continued for 8h. The reaction mixture was concentrated under reduced pressure and purified by reversed phase HPLC (column Reprosil-Pur C18-A9, 250×20 mm, gradient elution acetonitrile:water (2:1) – pure acetonitrile) followed by column chromatography on silica (eluent hexanes:ethyl acetate 3:1) to give 0.060 g (31%) of 4-{6-[3-(2,6-dichlorophenyl)-5-isopropyl-isoxazol-4-ylmethoxy]-2-trifluoromethyl-pyridin-3-ylsulfamoyl}-benzoic acid methyl ester as colourless oil.
The synthetic route of 69812-51-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Phenex Pharmaceuticals AG; EP1894924; (2008); A1;,
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