Scheme 2. Preparation of Carboxy- (9) and NHS-Functionalized (10) TDG Derivatives.
Reagents and conditions: (a) Na, THF, 0–25 °C, 39%; (b) CuI, CH3OH, 25 °C, 64%; (c) TFA/DCM, 25 °C, 98%; (d) TSTU, DiPEA, DMF, 25 °C.
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