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. 2019 Apr 1;11(4):151. doi: 10.3390/pharmaceutics11040151

Scheme 1.

Scheme 1

Synthesis of conjugates 10 and 11. Reagents and conditions: (a) 5 (1.1 eq), DIPEA (3 eq), DMF, RT, 5 h or 6 (3 eq), PyBOP (3 eq), HOBt (3.5 eq), DIPEA (3.5 eq), DMF, RT, 5 h; (b) 9 (1.1 eq), CuSO4·5H2O (0.5 eq), sodium ascorbate (0.6 eq), 1:1 DMF/H2O, 35 °C, 24 h.