Scheme 2.
Synthesis of Negative Control Compounds 27 and 28a
aReaction conditions: (a) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI), 1-hydroxy-7-azabenzo-triazole (HOAt), N-methylmorpholine (NMM), dimethyl sulfoxide (DMSO), rt, 4 h; (b) 13, EDCI, HOAt, NMM, DMSO, rt, 12 h; (c) K2CO3, CH3I, DMF, rt, 4 h; (d) TFA/DCM, rt, 30 min; (e) 14, EDCI, HOAt, NMM, DMSO, rt, 12 h.