1,2-Dichloroethane → 3-Oxo-2-[2-(pyrimidin-2-ylamino)ethyl]-2,3-dihydro-1H-isoindole-5-carbonyl-2(S)phenylsulfonylamino-beta-alanine t-butyl ester

Beteiligte Stoffe

Reaktionsschritte

A DMF solution (10 mL) of acid 6-4 (382 mg, 1.28 mmol) 1-4 (517 mg, 1.54 mmol), HOBT (264 mg, 1.13 mmol) NMM (563 μl, 5.1 mmol) and EDC (331 mg, 1.73 mmol) was stirred under ambient conditions for 18 h. The DMF was removed at 50° C. and the residue partitioned between EtOAc and H2O. The organic layer was washed with sat. NaHCO3 solution, brine, and dried (MgSO4). Evaporation gave a yellow foam which was purified by flash chromatography (silica, 3:1 acetone/CH2Cl2) to provide 6-5 as a colorless foam.

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