52201-28-2Relevant academic research and scientific papers
Method for preparing parecoxib sodium key intermediates
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Paragraph 0028; 0032, (2017/08/29)
The invention relates to a method for preparing parecoxib sodium key intermediates, and belongs to the field of medicine synthesis. The method for preparing the parecoxib sodium key intermediates includes steps of firstly, preparing 1-(1-methyl-2-styrene)-pyrrolidine (a compound I); secondly, preparing 5-methyl-3, 4-diphenyl-5-(pyrrolidine-1-base)-4, 5-dihydro-isoxazole (a compound II); thirdly, preparing a crude product of 5-methyl-3, 4-diphenyl isoxazole (a compound III); fourthly, refining a crude product of 5-methyl-3, 4-diphenyl-5-isoxazole (a compound III). The shortcomings of existing synthesis methods can be overcome by the aid of the method. The method for preparing the parecoxib sodium key intermediates has the advantages of mild reaction conditions, inexpensive and easily available raw materials, simplicity in after-treatment operation, short production cycle and high product purity and yield. Besides, the novel method is provided for preparing the parecoxib sodium key intermediates.
Easily available nickel complexes as catalysts for the intermolecular hydroamination of alkenes and alkynes
Reyes-Sanchez, Adan,Garcia-Ventura, Ilnett,Garcia, Juventino J.
, p. 1762 - 1768 (2014/01/06)
A series of nickel complexes of the type [(P-P)NiX2] ((P-P) = bisphospines or bisphosphites, X = chloride, triflate) were used as catalysts for the hydroamination of both activated and unactivated alkenes and alkynes with pyrrolidine. In general, the use of activated unsaturations, such as acrylonitrile, required mild reaction conditions (e.g. 100 °C and 4 h) in comparison with other non-activated alkenes. Particularly with a series of alkynes, the use of nickel(ii) centers diminished or even inhibited the formation of otherwise undesired homocoupling and/or transfer hydrogenation by-products, such as the ones obtained in the presence of zerovalent nickel. When using less activated substrates, better selectivity was obtained, although harsher reaction conditions were needed. From a general perspective, the results of this report strongly support the potential use of nickel as a good candidate for further application in the hydroamination of organic unsaturations by means of screening of several π acceptor ligands. The Royal Society of Chemistry.
Application of [3+2]-cycloaddition in the synthesis of valdecoxib
Reddy, Anumula Raghupathi,Goverdhan, Gilla,Sampath, Aalla,Mukkanti, Khagga,Reddy, Padi Pratap,Bandichhor, Rakeshwar
experimental part, p. 639 - 649 (2012/01/13)
A large scale synthesis of valdecoxib 1 is described. Our work features potential application of [3+2]-dipolar cycloaddition involving enamine and in situ-generated nitrile oxide derivatives. Dr. Reddy's Laboratories Ltd.
Method for preparing 3,4-diphenyl-substituted isoxazole compounds
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Page/Page column 8, (2008/06/13)
The present invention relates to a process for preparing diaryl-substituted isoxazole using compounds of Formula (V) and Formula (VII): where Y is and to processes for preparing valdecoxib and parecoxib.
