Urea Formation

(CDI)

Examples:

Example 1

To a solution of A (80 mg, 0.24 mmol) in DMF (2 mL) was added TEA (48 mg, 0.48 mmol). The resulting mixture was stirred at RT for 10 min, after which time was added CDI (39 mg, 0.24 mmol). The mixture was stirred at RT for 1 h, after which time was added B (48 mg, 0.48 mmol). The mixture was stirred at RT for another 12 h. The mixture was purified by Prep-HPLC [5-95% (ACN)/(0.5% NH3 in H2O)] to provide the product as a yellow solid. [68 mg, 52%]

[Patent Refernce: WO2015089337, page 98, (17.5 MB)]