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 431-38-9 as follows., 431-38-9
To a solution of racemic 3-azabicyclo[3.1.0]hexane-1,3-dicarboxylic acid-3-tert-butyl ester (200 mg, 0.88 mmol) in DMF (5 mL), TBTU (339 mg, 1.056 mmol) and TEA (160 muL, 1.14 mmol) are added. Mixture is stirred at room temperature for 10 min, then racemic 3-amino-1,1,1-trifluoro-2-propanol (125 mg, 0.97 mmol) is added and the mixture stirred at room temperature overnight. AcOEt and saturated NaHCO3 are added, the organic phases separated and washed with 10% citric acid and brine. The organic layer is then dried using a phase separator cartridge and evaporated under reduced pressure to furnish the title compound (330 mg, 90% content, 100%), that is used as such. HPLC-MS (Method 2): Rt=0.94 min. MS (ESI pos): m/z=339 (M+H)+
The chemical industry reduces the impact on the environment during synthesis 431-38-9, I believe this compound will play a more active role in future production and life.
Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; GIOVANNINI, Riccardo; BERTANI, Barbara; FERRARA, Marco; LINGARD, Iain; MAZZAFERRO, Rocco; ROSENBROCK, Holger; US2013/197011; (2013); A1;,
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