SÀ H activation reaction of thiols employing dibenzyl azodicarboxylate (DBAD) has been developed for the preparation of sulfenamides. The dehydrogenation of thiols and amines under these reaction conditions involved the formation of dibenzyl hydrazine-1,2-dicarboxylate (5 a), which led to the SÀ N bond formation reaction. The reaction proceeds efficiently with the release of 5 a and affords various sulfenamides in good to excellent yields.[a] S.
An efficient synthetic approach involving indole alkylation/Pictet-Spengler cyclization was developed to form benzazepinoindole derivatives. The reactions proceeded smoothly with indoles, 2-aminobenzyl alcohols, and aldehydes in the presence of TiCl 4 as a Lewis acid catalyst. The developed one-pot protocol is operationally simple and tolerates various functional groups. Furthermore, this mild and practical tandem reaction provides a direct route to access benzazepinoindole-containing natural products and bioactive compounds.[a] E.
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