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. 2019 Aug 23;14(18):1662–1668. doi: 10.1002/cmdc.201900370

Scheme 2.

Scheme 2

Reagents and conditions: a) (COCl)2, DMF, CH2Cl2, 2 h; b) methylisobutyrate, LDA, THF, −78 °C→RT, overnight; c) N2H4⋅H2O, EtOH, RT, 18 h, 16–64 % (over two steps); d) TBAB, aq. NaOH, CH2Cl2, 60 °C, 18 h, 38–69 %.