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. 2016 Apr 20;7(6):558–562. doi: 10.1021/acsmedchemlett.5b00234

Scheme 1. Synthesis of Piperazinylquinolines.

Scheme 1

Reagents and conditions: (a) 10, tert-butyl piperazine-1-carboxylate or 4-phenylpiperidine, DIPEA, toluene, reflux; (b) 11 or 1,3-diaminopropan-2-ol, neat, microwave, 100 to 160 °C; (c) HCl/EtOAc, 5 °C; (d) R2Cl, TEA, DCM, 0 °C to r.t..