74685-00-0Relevant articles and documents
Synthesis and biological activity of novel acyclic versions of neplanocin A
Wu, Ying,Hong, Joon Hee
, p. 517 - 521 (2005)
Novel acyclic Neplanocin A analogues were designed and synthesized. The coupling of the alkyl bromide 6 with nucleosidic bases (T, U, 5-FU, 5-IU, C, A) and desilylation afforded a series of novel acyclic nucleosides. The synthesized compounds 13-18 were evaluated for their antiviral and antitumor activity.
BICYCLIC SULFONAMIDES
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Paragraph 0186, (2020/08/28)
Provided herein are compounds of Formulae (I) and (II), or pharmaceutically acceptable salts of the foregoing, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein
Hydrogenative Cyclopropanation and Hydrogenative Metathesis
Peil, Sebastian,Guthertz, Alexandre,Biberger, Tobias,Fürstner, Alois
supporting information, p. 8851 - 8856 (2019/05/28)
The unusual geminal hydrogenation of a propargyl alcohol derivative with [CpXRuCl] as the catalyst entails formation of pianostool ruthenium carbenes in the first place; these reactive intermediates can be intercepted with tethered alkenes to give either cyclopropanes or cyclic olefins as the result of a formal metathesis event. The course of the reaction is critically dependent on the substitution pattern of the alkene trap.
One-Step Synthesis of 3,4-Disubstituted 2-Oxazolidinones by Base-Catalyzed CO2 Fixation and Aza-Michael Addition
Mannisto, Jere K.,Sahari, Aleksi,Lagerblom, Kalle,Niemi, Teemu,Nieger, Martin,Sztanó, Gábor,Repo, Timo
supporting information, p. 10284 - 10289 (2019/08/01)
2-Oxazolidinones are saturated heterocyclic compounds, which are highly attractive targets in modern drug design. Herein, we describe a new, single-step approach to 3,4-disubstituted 2-oxazolidinones by aza-Michael addition using CO2 as a carbonyl source and 1,1,3,3-tetramethylguanidine (TMG) as a catalyst. The modular reaction, which occurs between a γ-brominated Michael acceptor, CO2 and an arylamine, aliphatic amine or phenylhydrazine, is performed under mild conditions. The regiospecific reaction displays good yields (av. 75 %) and excellent functional-group compatibility. In addition, late-stage functionalization of drug and drug-like molecules is demonstrated. The experimental results suggest a mechanism consisting of several elementary steps: TMG-assisted carboxylation of aniline; generation of an O-alkyl carbamate; and the final ring-forming step through an intramolecular aza-Michael addition.
