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. Author manuscript; available in PMC: 2012 Aug 27.
Published in final edited form as: ChemMedChem. 2011 Jul 5;6(9):1593–1602. doi: 10.1002/cmdc.201100188

Scheme 1.

Scheme 1

Reagents and conditions: a) NaBH(OAc)3, HOAc, RT, 1 h; b) DDQ, THF, RT, 16 h; c) 1. (COCl)2, Et2O; 2. MeOH, 0°C → RT, 16 h; d) Ph3P=CHCO2Et, PhMe, 100°C, 16 h; e) NH (l), EtOH, 80° 3 C, 3 d; f) tBuOK, Et2O or THF, −20°C→RT, 16 h; g) TFA, CH2Cl2, RT, 2 h; h) R1CO2H, HOBt, EDC, DMAP, CH2Cl2, RT, 16 h; i) ArCHO or HCHO, NaBH(OAc)3, HOAc, THF, RT, 16 h.