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Table 1. Overview of the synthesized 1,2,5-benzothiadiazepin-4-on-1,1-dioxides. Yieldsare of purified material and are based upon the loading levels of the resin.O O OSNHR 1NR 2R 37 8R 1R 2Product Yield (%)a H Bn H H 26b Me Bn H H 38c (CH 2 ) 2 Ph Bn H H 54d i.Bu Bn H H 41e C 10 H 21 Bn H H 22f (CH 2 ) 2 N(CH 2 CH 2 )O Bn H H 33g H H H H 39h Me H H H 42i (CH 2 ) 2 Ph H H H 47j i.Bu H H H 32k C 10 H 21 H H H 10l (CH 2 ) 2 N(CH 2 CH 2 )O H H H 69m Me iBu H H 48n Me iBu Cl H 40o Me (CH 2 ) 4 NHBoc H H 54p Me CH 2 Im(Trt) H H 38q Me CH 2 indole(Boc) H H 57r Me Bn Cl H 23s Me Bn Br H 11t Me Bn H F 24u Me H Cl H 48v Me H Br H 56w Me H H F 61R 3Results and DiscussionIn Table 1 a list of synthesized benzothiadiazepines is outlined. Diversification of the targetheterocycles was achieved in three dimensions by using different amino acids (R 2 ),alcohols (R 1 ) and ortho-nosylchlorides (R 3 ).AcknowledgmentsWe would like to thank the “IWT - Agency for Innovation by Science and Technology” and GhentUniversity for financial support.References1. Evans, B.E., et al. J. Med. Chem. 31, 2235-2246 (1988).2. a) Horton, D.E., Bourne, G.T., Smythe, M.L. Chem. Rev. 103, 893-930 (2003); b) Costantino, L.,Barlocco, D. Curr. Med. Chem. 13, 65-85 (2006).3. a) Ogawa, K., Matsushita, Y. Chem. Pharm. Bull. 40, 2442-2447 (1992); b) Di Santo, R., Costi, R.,Artico, M., Ragno, R., Lavecchia, A., Novellino, E., Gavuzzo, E., La Torre, F., Cirilli, R., Cancio,R., Maga, G. Chem. Med. Chem. 1, 82-95 (2006).135