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Reagents and conditions: (a) tert-butyl (4-aminobutyl)carbamate or tert-butyl (5-aminopentyl)carbamate, DiPEA, MeCN, 70–85 °C, 46–74%; (b) TFA, quant; (c) 4-fluorosulfonylbenzoyl chloride, DiPEA, MeCN, 70 °C, 2–4%; (d) Boc2O, DCM, quant; (e) PPh3, CBr4, 90%; (f) propargylamine, DiPEA, 46%; (g) 4-fluorosulfonylbenzoyl chloride, DiPEA, MeCN, quant; (h) i. 5, TFA, DCM, ii. DiPEA, MeCN, 70 °C, 45%.
