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. 2016 Feb 25;59(10):4462–4475. doi: 10.1021/acs.jmedchem.5b01865

Scheme 1. Synthesis of 2.

Scheme 1

Reagents and conditions: (a) NaH, MeI, DMF, rt, 71%; (b) HNMe2·HCl, NaOAc, AcOH, NaBH(OAc)3, DCM, rt, 89%; (c) B2pin2, KOAc, Pd(dppf)Cl2, 1,4-dioxane, 90 °C, 63%; (d) Pd(dppf)Cl2·DCM, Na2CO3(aq), DMF, 100 °C, 17%