149489-04-3Relevant articles and documents
Development of a Novel Process for the Kilogram-Scale Synthesis of Spiro[1 H-pyrido[2,3- d][1,3]oxazine-4,4′-piperidine]-2-one
Mowrey, Dale R.,Reif, James J.,Milkiewicz, Karen L.,Allwein, Shawn P.
, p. 1236 - 1240 (2018)
Spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one (3) is a key building block in many biologically active compounds. The synthesis of this compound, as reported in the literature, is low-yielding. We have discovered and developed a robust, high-yielding process to generate 3 as a bis-HCl salt using alternative starting materials and reaction conditions. The developed process was successfully demonstrated on a kilogram scale. A two-batch kilo lab campaign generated the bis-HCl salt of 3 in >99 HPLC area percent purity and 77% overall yield.
Hydroarylation of Arenes via Reductive Radical-Polar Crossover
Flynn, Autumn R.,Mcdaniel, Kelly A.,Hughes, Meredith E.,Vogt, David B.,Jui, Nathan T.
supporting information, p. 9163 - 9168 (2020/07/10)
A photocatalytic system for the dearomative hydroarylation of benzene derivatives has been developed. Using a combination of an organic photoredox catalyst and an amine reductant, this process operates through a reductive radical-polar crossover mechanism where aryl halide reduction triggers a regioselective radical cyclization event, followed by anion formation and quenching to produce a range of complex spirocyclic cyclohexadienes. This light-driven protocol functions at room temperature in a green solvent system (aq. MeCN) without the need for precious metal-based catalysts or reagents or the generation of stoichiometric metal byproducts.
Method for inhibition of HIV related viruses
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, (2008/06/13)
Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.