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. Author manuscript; available in PMC: 2019 Nov 9.
Published in final edited form as: J Med Chem. 2018 Jun 29;61(13):5623–5642. doi: 10.1021/acs.jmedchem.8b00375

Scheme 3.

Scheme 3.

Synthesis of 6a–6e.

(a) PdCl2(dppf)CH2Cl2, ArB(OH)2 or ArBpin, CH3CN, aq. K2CO3, 95 °C, 1–16 h; (b) (R)-(+)-2-methyl-2-propanesulfinamide, Ti(OEt)4 THF, reflux, 16 h; then (c) NaBH4, THF, −60 °C to rt (58–62%); (d) 4.0 M HCl, MeOH, rt (95–97%); (e) R2COCl, Et3N, CH2Cl2, rt, 2 h or R2CO2H, HATU, DMF, rt, 16–40 h.