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. 2019 Oct 10;10(11):1524–1529. doi: 10.1021/acsmedchemlett.9b00325

Scheme 1.

Scheme 1

Reagents and conditions: (a) Zn, I2, Pd2(dba)3, N-Boc-3-iodoazetidine, tri(o-tolyl)phosphine, DMF, 50 °C, 90 min (Compounds 8 and 9); (b) Zn, I2, Pd2(dba)3, N-Boc-3-iodoazetidine, tri-2-furylphosphine; (c) benzophenonimine, sodium tert-butoxide, Pd2(dba)3, toluene, 100 °C, 3 h, then 50% hydroxylamine in water, MeOH, 25 °C, 18 h; (d) TFA, DCM, 25 °C, 3 h.