Design and synthesis of cyclic sulfonamides and sulfamates as new calcium sensing receptor agonists
作者:Lionel Kiefer、Tatiana Gorojankina、Philippe Dauban、Hélène Faure、Martial Ruat、Robert H. Dodd
DOI:10.1016/j.bmcl.2010.10.006
日期:2010.12
The design, synthesis and calcimimetic properties of various cyclic sulfonamides and sulfamates are described. The latter were prepared from the corresponding o-alkenylarenesulfonamides via copper-or rhodium-catalyzed intramolecular aziridination. The size of the cyclic sulfonamide rings as well as the position of the crucial (R)-naphthylethylamine substituent significantly affected calcimimetic activity. The most active compounds were the six-and seven-membered sulfonamides 30a and 31a and sulfamate 34a. (C) 2010 Elsevier Ltd. All rights reserved.