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. Author manuscript; available in PMC: 2019 Sep 27.
Published in final edited form as: J Med Chem. 2018 Sep 7;61(18):8299–8320. doi: 10.1021/acs.jmedchem.8b00838

Scheme 3. Synthesis of 2-Aminopyrimidinyl Derivative 41a.

Scheme 3.

aReagents and conditions: (a) (Boc)2O, CH2Cl2, DIPEA, DMAP, rt, 16 h, 85%; (b) Pd/C, H2 (1 atm), MgO, MeOH, rt, 48 h, 92%; (c) N-bromosuccinimide, CH2Cl2, rt, 5 h, 60%; (d) 2-aminopyrimidine, Pd2(dba)3/Xantphos, 1,4-dioxane, Cs2CO3, 100 °C, 18 h, 30%; (e) TFA, CH2Cl2, rt, 16 h, 98%; (f) guanidine (2 M in MeOH), DMF, rt, 35%.