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. 2021 Dec 15;26(24):7599. doi: 10.3390/molecules26247599

Scheme 1.

Scheme 1

18 was prepared using the procedure described in ref. 30. (a) 19 (1 eq.), 20 (1.5 eq), CuI (0.1 eq), (PPh3)2PdCl2 (0.2 eq), Et3N (0.25 M), 80 °C, 51%; (b) Pd(OH)2 (20% on carbon) (0.3 eq.), EtOH (0.1 M), H2 atm.; (c) CH2Cl2 (0.04 M), trifluoroacetic acid (TFA) (10% v/v); (d) 24 (1.1 eq), HATU (1.1 eq.), DIPEA (3 eq.), DMF (0.2 M), 32% 25 over three steps, 1% 10 over three steps.