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. 2024 Apr 30;67(16):13550–13571. doi: 10.1021/acs.jmedchem.3c02469

Scheme 2. Synthesis of 8.

Scheme 2

Reagents and conditions: (a) HATU, i-Pr2NEt, DMF, 93%; (b) 4 M HCl in dioxane; (c) N-Boc-l-tert-leucine, HATU, i-Pr2NEt, DMF, 75% over two steps; (d) CF3CO2CH2CH3, i-Pr2NEt, CH3OH; (e) Burgess reagent, DCM 29% over three steps.