Rolfe, AlanYoung, KyleVolp, KellySchoenen, Frank J.Neuenswander, BenjaminLushington, Gerald H.Hanson, Paul R.2017-05-222017-05-222009Rolfe, A., Young, K., Volp, K., Schoenen, F., Neuenswander, B., Lushington, G. H., & Hanson, P. R. (2009). A One-Pot, 3-Component, Domino Heck-aza-Michael Approach to Libraries of Functionalized 1,1-Dioxido-1,2-benzisothiazoline-3-acetic acids. Journal of Combinatorial Chemistry, 11(4), 732–738. http://doi.org/10.1021/cc900025ehttps://hdl.handle.net/1808/24255This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Combinatorial Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://doi.org/10.1021/cc900025e.A sequential three-component synthesis of functionalized benzisothiazoline-3-acetic acid 1,1- dioxides utilizing a domino Heck-aza-Michael pathway is reported. This one-pot procedure rapidly assembles functionalized benzylsulfonamides, which undergo a palladium-catalyzed, domino, Heckaza- Michael transformation in an experimentally straightforward manner. This attractive protocol has been utilized to synthesize three combinatorial sub-libraries (I-III) comprising a total of 95 compounds in high purities (≥95% for 75 compounds), yield and quantities.Copyright © American Chemical SocietyDominoHeckAza-MichaelSultamArticle10.1021/cc900025ePMC2895961openAccess