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. Author manuscript; available in PMC: 2020 Feb 14.
Published in final edited form as: J Med Chem. 2019 Jan 24;62(3):1562–1576. doi: 10.1021/acs.jmedchem.8b01754

Scheme 2.

Scheme 2.

aSynthesis of Compounds 3, 19, 22–31

R2 = (o) 5-(2-methoxypyrimidine), (p) cyclopropyl, (q) 3-pyridine, (r) 4-pyridine, (s) 5-pyrimidine, (t) 4-pyridazine, (u) 5-(2-methylpyrimidine), (v) 5-(2-trifluoromethylpyrimidine), (w) 5-(2-cyclopropylpyrimidine), (x) 2-pyridine, (y) 2-pyrimidine and (z) 2-pyrazine.

a Reagents and conditions: (a) Pd(PPh3)4, R2-B(OH)2 (39o-w), Cs2CO3, Dioxane/H2O, 110 °C; or (b) Pd2(dba)3, Sn(nBu)3-R2 (40x-z), Xphos, dioxane, 100 °C