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. 2024 Feb 8;67(4):2849–2863. doi: 10.1021/acs.jmedchem.3c01976

Scheme 2. Synthetic Routes of R2 Analogue 11 and R3 Analogue 15.

Scheme 2

Reagents and conditions: (i) MeI, K2CO3, DMF, 60 °C, 1 h, 23% for 8 and 26% for 12; (ii) 7 M NH3 in MeOH, RT, 16 h; (iii) 10% Pd/C, H2 (g), EtOH, 60 °C, 16 h, two-step yield 92% for 10 and 96% for 14; (iv) 4-fluorobenzoic acid, TEA, PyBrop, DCE, MW 120 °C, 20 min; (v) KOtBu, iPrOH, MW 130 °C, 30 min, two-step yield 73% for 11 and 76% for 15.