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. Author manuscript; available in PMC: 2017 Jan 12.
Published in final edited form as: Bioorg Med Chem. 2014 Apr 24;22(12):3083–3090. doi: 10.1016/j.bmc.2014.04.030

Scheme 4.

Scheme 4

(a) LDA, THF, −78°C, 15 min; (b) R1-X, −78°C-rt, 16 h, 67–75%; (c) R2-X, 78°C-rt, 16 h, 29–58%; (d) LAH, THF, 70°C, 16 h; (e) PMPCH(OMe)2, CSA, DCM, rt, 4 h, 50–86% over 2 steps; (f) DMP, DCM, rt, 2 h; (g) NaClO2, NaHPO4, acetone, DCM, H2O, rt, 15 min; (h) piperidine, DMF, rt, 30 min; (i) EDC, DIPEA, HOBt, THF, rt, 16 h, 42–51% over 4 steps; (j) 80% AcOH, rt, 16h, 64–81%.