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. Author manuscript; available in PMC: 2018 Apr 12.
Published in final edited form as: ChemMedChem. 2017 Nov 24;12(23):1942–1952. doi: 10.1002/cmdc.201700614

Scheme 3.

Scheme 3

Reagents and conditions: a) TosMIC, K2CO3, MeOH, 55°C, 1.5 h, 96%; b) TFA, CH2Cl2, 23°C, 2.5 h; c) 6, N,N-DIPEA, MeCN, 23°C, 4–7 days, 47–80% (over two steps); d) iPrMgCl, dry THF, 15°C, 40 min, then AcN(-Me)OMe, −15°C→23°C, 5 h, 79%; e) RuCl[(−R,R)-TsDPEN](mesitylene) for 3k or RuCl(p-cymene)[(S,S)-Ts-DPEN] for 3l, TEA, HCOOH, dry CH2Cl2, 0°C→23°C, 7 h, 95–97%.