o-Toluenesulfonyl chloride → HCID 19705505, compound

Participants

Reaction Conditions

Reaction Steps

Toluenesulfonyl chloride (372 mg) is added to a solution of tert-butyl α-(2-aminoethyl)-3-(2-methylpropyl)-2-oxo-1-(2-phenylethyl)-3-pyrrolidineacetate (EXAMPLE 73, step 1; 654 mg, 1.62 mmol), CH2Cl2 (10.0 mL), and diisopropylethylamine (0.34 mL) at 0° C. The solution is stirred at 0° C. for 1 hour and at room temperature for 16 hours. Basic workup (CH2Cl2, NaHCO3, MgSO4) and purification by flash chromatography gives 634 nag (70%) of the title compound as a white solid (mp 136°-138° C.):

Provenance & Evidence