title: Microwave-assisted preparation of 4-amino-3-cyano-5-methoxycarbonyl-N-arylpyrazoles as building blocks for the diversity-oriented synthesis of pyrazole-based polycyclic scaffolds.
abstract: The synthesis of 4-amino-3-cyano-N-arylpyrazoles A based on a Thorpe-Ziegler cyclization as the key step has been achieved using microwave activation. Via a new diversity-oriented synthetic pathway, these highly functionalized building blocks allowed the access to various heteroaromatic scaffolds such as pyrazolo-pyridines B, pyrazolo-pyrimidines C and pyrazolo-oxadiazoles D. Interestingly, these platforms contain three to four reactive sites that could be used for post-functionalization in order to further increase the molecular diversity.
authors.affiliation: Université Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Pères, 75006 Paris, France. patricia.busca@parisdescartes.fr.
authors.forename: Laurent
authors.initials: L
authors.lastname: Le Corre
authors.forename: Lotfi
authors.initials: L
authors.lastname: Tak-Tak
authors.forename: Arthur
authors.initials: A
authors.lastname: Guillard
authors.forename: Guillaume
authors.initials: G
authors.lastname: Prestat
authors.forename: Christine
authors.initials: C
authors.lastname: Gravier-Pelletier
authors.forename: Patricia
authors.initials: P
authors.lastname: Busca
mesh_terms: D009682:Magnetic Resonance Spectroscopy; D008872:Microwaves; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D011720:Pyrazoles