These common heterocyclic compound, 15441-10-8, name is 3-(Aminosulfonyl)propanoic acid, 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. name: 3-(Aminosulfonyl)propanoic acid
General procedure: To a solution of 3-(4-((2-aminopropyl)thio)-1 ,2,5-oxadiazol-3-yl)-4-(3-(difluoromethyl)-4- fluorophenyl)-1 ,2,4-oxadiazol-5(4H)-one hydroiodide (Int 102) (416 mg, 0.81 mmol), HATU (462 mg, 1 .22 mmol) and Et3N (245 mg, 2.43 mmol) in DMF (8 mL) 2- sulfamoylacetic acid (135 mg, 0.97 mmol) was added and the mixture was stirred at rt overnight. EtOAc (20 mL) was added and the mixture was extracted with water (2 x 20 mL). The combined organic layers were dried over anhydrous Na2S0 , filtered and concentrated to dryness. The residue was purified by column chromatography to give the title compound as a white solid.
The synthetic route of 3-(Aminosulfonyl)propanoic acid has been constantly updated, and we look forward to future research findings.
Reference:
Patent; PHENEX DISCOVERY VERWALTUNGS-GMBH; STEENECK, Christoph; KINZEL, Olaf; ANDERHUB, Simon; HORNBERGER, Martin; KLEYMANN, Gerald; HOFFMANN, Thomas; (191 pag.)WO2018/83241; (2018); A1;,
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