title: Continuous flow thermolysis of azidoacrylates for the synthesis of heterocycles and pharmaceutical intermediates.
abstract: An efficient, safe and scalable procedure for the continuous flow thermolysis of azidoacrylates to yield indoles has been developed and was applied to the synthesis of related heterocycles. The scalability of the process was demonstrated in the continuous flow synthesis of a precursor to the DAAO inhibitor 4H-furo[3,2-b]pyrrole-5-carboxylic acid.
authors.affiliation: Max Planck Institute of Colloids and Interfaces, Department of Biomolecular Systems, Potsdam, Germany.
authors.forename: Alexander G
authors.initials: AG
authors.lastname: O'Brien
authors.forename: François
authors.initials: F
authors.lastname: Lévesque
authors.forename: Peter H
authors.initials: PH
authors.lastname: Seeberger
mesh_terms: D000179:Acrylates / Q000737:chemistry*; D001386:Azides / Q000737:chemistry; D003605:D-Amino-Acid Oxidase / Q000037:antagonists & inhibitors / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D006868:Hydrolysis; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry*; D011392:Proline / Q000031:analogs & derivatives
chemical_list: D000179:Acrylates; D001386:Azides; D004791:Enzyme Inhibitors; D007211:Indoles; D011392:Proline; D003605:D-Amino-Acid Oxidase