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. Author manuscript; available in PMC: 2020 Mar 5.
Published in final edited form as: ChemMedChem. 2019 Feb 5;14(5):545–560. doi: 10.1002/cmdc.201800725

Scheme 2.

Scheme 2.

Reagents and conditions. a) R2CH2P+Ph3Br−, nBuLi, dry THF, 1 h, −78 °C; b) (CH3CN)2Cl2Pd, CHCl3, 72 h, 25 °C, 69–84% (2 steps); c) AD-mix-α t-BuOH/H20, 24 h, 25 °C, 68–73%; d) TEA, thionyl chloride, 0 °C, 45 min, 66–79%; e) NaN3, DMF, 10 h, 80 °C, 74–88%; f) (Boc)2O, H2, Pd/C, EtOAc, 1 atm, 25 °C, 15 h; g) TFA, dry CH2Cl2, 1 h, from 0 °C to 25 °C, 66–86% (2 steps).