12 research outputs found
Magnetic bottle configuration to coat 1.3 GHz copper cavities with a Nb sputtered film
Submitted to Nucl. Instr. & Meth. in Phys. ResConsiglio Nazionale delle Ricerche (CNR). Biblioteca Centrale / CNR - Consiglio Nazionale delle RichercheSIGLEITItal
Synthesis of the ortho/meta/para Isomers of relevant pharmaceutical compounds by coupling a sonogashira reaction with a regioselective hydration
This document is the Accepted Manuscript version of a Published Work that appeared in final form in
ACS Catalysis, copyright © American Chemical Society after peer review and technical editing by the publisher.Aryl ketones substituted in ortho, meta, and
para position are prepared by a palladium-catalyzed Sonogashira
reaction followed by a regioselective hydration of the soformed
alkyne with triflimidic acid or a gold catalyst, under
catalytic conditions. This methodology opens a way to obtain
substituted aryl alkyl ketones from readily available starting
materials, haloarenes, and terminal alkynes. The syntheses of
the different regioisomers of haloperidol, melperone, pipamperone,
and ibuprofen are presented. Structure−activity relationships for these compounds are studied with dopaminergic and
cyclooxigenase binding assays.Financial support by the Severo Ochoa program and Consolider-Ingenio 2010 (proyecto MULTICAT) from MCIINN is acknowledged, and also to the King Saud University. A.L.-P. thanks ITQ for a contract. J.R. C.-A. and P.R.M. thank MCIINN for the concession of a FPU contract.Leyva Perez, A.; Cabrero Antonino, JR.; Rubio Marqués, P.; Al-Resayes, SI.; Corma Canós, A. (2014). Synthesis of the ortho/meta/para Isomers of relevant pharmaceutical compounds by coupling a sonogashira reaction with a regioselective hydration. ACS Catalysis. 4(3):722-731. https://doi.org/10.1021/cs401075zS7227314