6164-77-8Relevant articles and documents
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Fleischer,Lawson
, p. 2772,2773 (1972)
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Quaternary Stereogenic Centers through Enantioselective Heck Arylation of Acyclic Olefins with Aryldiazonium Salts: Application in a Concise Synthesis of (R)-Verapamil
Oliveira, Caio C.,Pfaltz, Andreas,Correia, Carlos Roque Duarte
supporting information, p. 14036 - 14039 (2016/01/25)
We describe herein a highly regio- and enantioselective Pd-catalyzed Heck arylation of unactivated trisubstituted acyclic olefins to provide all-carbon quaternary stereogenic centers. Chiral N,N ligands of the pyrimidine- and pyrazino-oxazoline class were developed for that purpose, providing the desired products in good to high yields with enantiomeric ratios up to >99:1. Both linear and branched substituents on the olefins were well-tolerated. The potential of this new method is demonstrated by the straightforward synthesis of several O-methyl lactols and lactones containing quaternary stereocenters, together with a concise enantioselective total synthesis of the calcium channel blocker verapamil.
Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase
Verschueren, Wim G.,Dierynck, Inge,Amssoms, Katie I. E.,Hu, Lili,Boonants, Paul M. J. G.,Pille, Geert M. E.,Daeyaert, Frits F. D.,Hertogs, Kurt,Surleraux, Dominique L. N. G.,Wigerinck, Piet B. T. P.
, p. 1930 - 1940 (2007/10/03)
Human immunodeficiency virus type-1 integrase is an essential enzyme for effective viral replication and hence a valid target for the design of inhibitors. We report here on the design and synthesis of a novel series of phthalimide analogues as integrase