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. 2015 Sep 29;58(19):7695–7706. doi: 10.1021/acs.jmedchem.5b00596

Scheme 1.

Scheme 1

Conditions: (a) R1CO2H (1 equiv), TBTU, (1 equiv), DIPEA, DCM, room temperature, 2 h or R1COCl (1 equiv), TEA, DCM, 0 °C to room temperature, 2 h; (b) R2NH2 (2 equiv), TBTU, (1 equiv), DIPEA, room temperature, 2 h, 2–85% yield for steps (a) and (b) combined. R1 and R2 are the substituents, as exemplified in Tables 1 and 36.