213025-72-0Relevant academic research and scientific papers
Substituted Pyrrololactams via Ring Expansion of Spiro-2H-pyrroles from Intermolecular Alkyne-Isocyanide Click Reactions
George, Jimil,Kim, Hun Young,Oh, Kyungsoo
supporting information, p. 628 - 631 (2017/02/10)
The facile synthesis of 6- to 8-membered pyrrololactams has been developed using a ring expansion of spiro-2H-pyrroles, the products of intermolecular alkyne-isocyanide click reactions. The key to successful ring expansion of spiro-2H-pyrroles to pyrrololactams is the enforced orbital overlap between the internal alkene and the amide carbonyl group through the conformationally locked bicyclic structures. The newly disclosed α-isocyano lactams, substrates for click reactions, should find their utility in the synthesis of pharmaceutically important heterocyclic compounds.
Facile synthesis of versatile functionalized amino caprolactams using RCM reactions of α-amino acrylamide
Liu, Gang,Tai, Wan-Yi,Li, Yu-Lin,Nan, Fa-Jun
, p. 3295 - 3298 (2007/10/03)
We report an efficient synthetic methodology allowing access to functionalized α-amino caprolactams using ring-closing metathesis (RCM). A very high tolerance of α-amino acrylamide RCM precursors toward functional groups is demonstrated. The synthetic pat
Parallel liquid synthesis of N,N′-disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors
Le Diguarher, Thierry,Ortuno, Jean-Claude,Dorey, Gilbert,Shanks, David,Guilbaud, Nicolas,Pierre, Alain,Fauchere, Jean-Luc,Hickman, John A.,Tucker, Gordon C.,Casara, Patrick J.
, p. 3193 - 3204 (2007/10/03)
A rapid structure-activity study was performed by parallel liquid synthesis on N,N′-disubstitution of 3-amino azepin-2-one to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities. The activities of the selected compounds were validated in vivo, and compounds 41a and 44a presented significant antitumour activity.
