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Unexpected reversible nitrogen atom transfer in the synthesis of polysubstituted imides and 7-aza-hexahydroindolones via enaminonitrile γ-lactams

✍ Scribed by Nabila Oukli; Sébastien Comesse; Nafa Chafi; Hassan Oulyadi; Adam Daïch


Book ID
104096205
Publisher
Elsevier Science
Year
2009
Tongue
French
Weight
531 KB
Volume
50
Category
Article
ISSN
0040-4039

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✦ Synopsis


An effective route to novel polysubstituted imides is described, which involves the reaction of enaminonitrile c-lactams derived from N-alkylated a-bromoacetamides and malononitrile with acryloyl chloride derivatives. This preceded via a sequence 1,4-addition-intramolecular peptidic coupling and a c-lactam hydrolysis in a one 'pot-procedure'. These imides were regioselectively reduced into corresponding Nacyliminium precursors, which subsequently submitted to an intramolecular aza-cyclization in acidic medium to provide novel 7-hexahydro-aza-indoles.