13154-14-8Relevant articles and documents
Development of a scalable process for DG-041, a potent EP3 receptor antagonist, via tandem heck reactions
Zegar, Siead,Tokar, Christopher,Enache, Livia A.,Rajagopol, Venkat,Zeller, Wayne,O'Connell, Matthew,Singh, Jasbir,Muellner, Frank W.,Zembower, David E.
, p. 747 - 753 (2007)
DG-041 is a small molecule antagonist of the EP3 receptor for prostaglandin E2 that is in clinical development for treatment of peripheral artery disease (PAD). Originally produced using a six-step synthetic procedure, process optimization led to development of a four-step sequence that is readily scalable. The key step in the optimized sequence contains two sequential Heck reactions, involving an intramolecular Heck cyclization followed by an intermolecular Heck coupling, performed in one pot to produce a highly substituted indole core.
Active Magnesium from Catalytically Prepared Magnesium Hydride or from Magnesium Anthracene and its Uses in the Synthesis
Bartmann, Ekkehard,Bogdanovic, Borislav,Janke, Nikolaus,Liao, Shijan,Schlichte, Klaus,et al.
, p. 1517 - 1528 (2007/10/02)
Highly reactive, pyrophoric forms of magnesium with specific surface areas of 20-109 m2/g (Mg*) can be generated by the dehydrogenation of catalytically prepared magnesium hydride (MgH2*) or by decomposition of magnesium anthracene * 3 THF (4).The decomposition of 4, with recovery of anthracene and THF, may be accomplished both thermally and by ultrasound in an organic solvent (toluene, n-heptane) or thermally in the solid state in vacuo.Mg* obtained by the latter method exhibits only weak reflections in the X-ray powder diagram and has, in comparison to other mentioned Mg* species, the highest reactivity toward hydrogen.Diverse Grignard compounds can be prepared under mild conditions (* from MgH2* or 4.The cleavage of THF with formation of 1-oxa-2-magnesiacyclohexane (2) is possible by employing Mg* from NgH2* or 4.
