with nitriles has been achieved by using rare‐earth complexes. This reaction is equivalent to the desired intramolecular hydroamination of alkenylamidines, and allows a new direct access to substituted 2‐imidazolines and tetrahydropyrimidines in high yields under operationally simple reaction conditions. Moreover, the methodology is also efficient for synthesis of symmetric and unsymmetric bridged diimidazolines
The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.
Stereoselective synthesis of tetrahydro-2H-[2]benzopyrano[3,4-c]pyrrol-3-ones and related compounds as precursors of serotonin 5-HT2C receptor agonists
作者:Stuart Francis、Takao Kiyoi、Mark Reid、Keneth Davies、Steven Laats、Duncan McArthur、Helen Feilden、Anna Marie Easson、Yasuko Kiyoi、Grant Wishart、Peter Ray
DOI:10.1016/j.tetlet.2011.03.053
日期:2011.7
Tetrahydro-2H-[2]benzopyrano[3,4-c]pyrrol-3-ones and the related 3a-methyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]isoindole analogues were synthesised by an intramolecular Diels-Alder reaction. The observed stereoselectivity was dependent upon the nature of the tethered dienophile as well as the judicious placement of the amide. (C) 2011 Published by Elsevier Ltd.
US8729274B2
申请人:——
公开号:US8729274B2
公开(公告)日:2014-05-20
Cycloisomerization of Olefins in Water
作者:Jeishla L. M. Matos、Samantha A. Green、Yuge Chun、Vuong Q. Dang、Russell G. Dushin、Paul Richardson、Jason S. Chen、David W. Piotrowski、Brian M. Paegel、Ryan A. Shenvi
DOI:10.1002/anie.202003948
日期:2020.7.27
one another, but unreactive with biopolymers and water, is challenging. Shown here are cobalt catalysts that react with alkenes under dilute, aqueous, buffered conditions and promote efficient cycloisomerization and formal Friedel–Crafts reactions. The constraining conditions of bioorthogonal chemistry are beneficial for reaction efficiency as superior conversion at low catalyst concentration is obtained