Research Article

Synthesis of New Fused Benzothiadiazepines and Macrocyclic Sulfamides Starting from N,N-Disubstituted Sulfamides and N(Boc)-Sulfamides

Scheme 1

General synthesis of bis sulfamides and N(Boc)-sulfamides. Reagents and conditions: (a) SO2Cl2 (1/4 equiv), CH2Cl2, 24 h (b) tert-BuOH, CH2Cl2, 0°C (c) Amine, TEA, CH2Cl2, 0°C to rt (d) α-amino ester, TEA (2 equiv), CH2Cl2, 0°C to rt (e) diamine (0.5 equiv), TEA (1 equiv), CH2Cl2, 0°C to rt.
810938.sch.001