60301-20-4Relevant academic research and scientific papers
Site-selective arene C-H amination via photoredox catalysis
Romero, Nathan A.,Margrey, Kaila A.,Tay, Nicholas E.,Nicewicz, David A.
, p. 1326 - 1330 (2015/10/12)
Over the past several decades, organometallic cross-coupling chemistry has developed into one of the most reliable approaches to assemble complex aromatic compounds from preoxidized starting materials. More recently, transition metal-catalyzed carbon-hydrogen activation has circumvented the need for preoxidized starting materials, but this approach is limited by a lack of practical amination protocols. Here, we present a blueprint for aromatic carbon-hydrogen functionalization via photoredox catalysis and describe the utility of this strategy for arene amination. An organic photoredox-based catalyst system, consisting of an acridinium photooxidant and a nitroxyl radical, promotes site-selective amination of a variety of simple and complex aromatics with heteroaromatic azoles of interest in pharmaceutical research. We also describe the atom-economical use of ammonia to form anilines, without the need for prefunctionalization of the aromatic component.
A method for the regioselective synthesis of 1-alkyl-1H-indazoles
Liu, Han-Jun,Hung, Shiang-Fu,Chen, Chuan-Lin,Lin, Mei-Huey
, p. 3907 - 3912 (2013/06/27)
A method for the regioselective synthesis of 3-unsubstituted 1-alkyl-1H-indazoles, starting with 2-halobenzonitriles and N-alkylhydrazines, is described. The two-step reaction pathway proceeds through the intermediacy of 1-alkyl-3-amino-1H-indazoles follo
TRPV1 Antagonists
-
Page/Page column 35, (2012/10/08)
Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
A general, one-step synthesis of substituted indazoles using a flow reactor
Wheeler, Rob C.,Baxter, Emma,Campbell, Ian B.,MacDonald, Simon J. F.
experimental part, p. 565 - 569 (2011/12/02)
Flow chemistry is a rapidly emerging technology within the pharmaceutical industry, both within medicinal and development chemistry groups. The advantages of flow chemistry, increased safety, improved reproducibility, enhanced scalability, are readily apparent, and we aimed to exploit this technology in order to provide small amounts of pharmaceutically interesting fragments via a safe and scalable route, which would enable the rapid synthesis of multigram quantities on demand. Here we report a general and versatile route which utilises flow chemistry to deliver a range of known and novel indazoles, including 3-amino and 3-hydroxy analogues.
BICYCLIC PYRIMIDINONES AND USES THEREOF
-
Page/Page column 131-132, (2008/12/06)
The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compoundof Formula I is also provided.
