1257872-22-2Relevant academic research and scientific papers
Regioselective synthesis of the 1-bromo-4-phenyl-tetrahydro-7-amino- benzocyclohepten-6-one, a subnanomolar aminopeptidase-N/CD13 inhibitor
Al-Lakkis-Wehbe, Mira,Roux, Lionel,Charrier, Cédric,Alavi, Sarah,Le Nou?n, Didier,Defoin, Albert,Tarnus, Céline,Albrecht, Sébastien
experimental part, p. 6447 - 6455 (2012/08/28)
A regioselective synthesis of the title 1-bromo-4-phenyl-tetrahydro-7- amino-benzocyclohepten-6-one 2 has been pursued and develop in order to allow a large scale synthesis of this highly potent and selective APN inhibitor (K i 60 pM). The pivo
Iodine(III)-mediated ring expansion: An efficient and green pathway in the synthesis of a key precursor for the design of aminopeptidase (APN or CD13) inhibitors
Roux, Lionel,Charrier, Cédric,Defoin, Albert,Bisseret, Philippe,Tarnus, Céline
experimental part, p. 8722 - 8728 (2011/01/04)
Iodine(III)-mediated ring expansion of a methylidenebenzocyclohexane derivative into the corresponding benzosuberone was used as a key reaction for the obtention of an important precursor for the design of aminopeptidase (APN or CD13) inhibitors. It represents the first application of this environmentally friendly rearrangement to medicinal chemistry.
