Skip to main content
. 2016 Jan 20;7(3):324–329. doi: 10.1021/acsmedchemlett.5b00472

Scheme 2. Synthesis of 3–25 (General Method 2).

Scheme 2

Reagents and conditions: (a) R1–OH, NaOH, CHCl3, 0–40 °C, 25–50%; (b) 32, DMF/DCM (1:1), HATU, DIPEA, 45 °C, 12 h, 40–60%; (c) DCM, TMS-I, 0 °C, 5 h, (100% crude yield); (d) DMF/DCM (1:1), HATU, DIPEA, 45 °C, 12 h, 40–80%; (e) H2, Pd/C, EtOH; (f) final deprotection step and Chiralcel OD column purification.