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. 2021 Aug 2;64(15):11288–11301. doi: 10.1021/acs.jmedchem.1c00663

Scheme 2. Reagents and Conditions.

Scheme 2

(a) Ethyl 4-isocyanatobenzoate, TEA, THF, room temp., 3 h, 42%; (b) 1 N NaOH, THF, 60 °C, 0.5 h, 63%; (c) l-glutamic acid di-tert-butyl ester hydrochloride, HATU, TEA, DMF, 25 °C, 8 h, 58%; and (d) TFA, 25 °C, 0.5 h, 75%.