Scheme 3.
Reagents and conditions: (a) NsCl, pyridine, 88%; (b) BocNH(CH2)3Br, K2CO3, DMF, 50 °C; then PhSH, 79%; (c) Propargylbromide, DIEA, DMF, 82%; (d) 6, Pd(PPh3)4, CuI, NEt3, THF, 60 °C, 63%; (e) 28% NH4OH, MeOH; TFA/H2O, 61% in two steps.
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