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. 2020 Nov 6;11(12):2510–2518. doi: 10.1021/acsmedchemlett.0c00496

Scheme 2. Synthesis of Final Compounds 18 and 19.

Scheme 2

Reagents and conditions: (m) HATU, DIEA, DMF, rt, 35%; (n) K2CO3, iPrOH, 100 °C, 51%; (o) 5-methyl-1H-tetrazole, dibenzyl diisopropylphosphoramidite, DCM, 0 °C – rt; (p) 35% H2O2 in water, DCM, 0 °C, 89% for two steps o & p; (q) H2, Pd–C, MeOH/EtOAc, rt, 78%.