151670-13-2Relevant academic research and scientific papers
Synthetic method for antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane
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Paragraph 0011; 0040, (2016/10/07)
The invention discloses a synthetic method for an antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane. The synthetic method comprises the following steps: (1) reacting a compound IV with a Grignard reagent to obtain a compound III; (2) employing a one-pot reaction to react the compound III with trimethylsulfoxonium iodide and 1,2,4-triazole and then react with p-toluenesulfonic acid, so as to obtain a compound II; and (3) reacting the compound II with methanesulfonyl chloride under an alkali condition to generate the target compound I, wherein the Grignard reagent is 2,4-difluorophenylmagnesium bromide or 2,5-difluorophenylmagnesium bromide, and the structural formula of the compound IV is shown in the specification. According to the synthetic route, the reaction conditions are mild and easy to control, the reaction route is simple, the related solvents in the reaction process all are common solvents, the reaction conversion rate is high, and the method possesses extremely high feasibility, is beneficial for industrialized batch production, and possesses extremely large exploitation potential and extremely good application prospect.
Triazole intermediate (D)-1-(1-cycloalkyl secondary amino)-2-(2-tetrahydropyranyl)oxo-1-acetone compounds and synthetic method
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Paragraph 0012, (2016/10/10)
The invention discloses triazole intermediate (D)-1-(1-cycloalkyl secondary amino)-2-(2-tetrahydropyranyl)oxo-1-acetone compounds, and the general formula of the compounds is shown in the specification, and in the formula, n is equal to 1-5. A preparation method of the compounds I comprises the following steps: (1) under protection of N2, reacting methyl D-lactate with cycloalkyl secondary amine at 30-60 DEG C by taking cycloalkyl secondary amine as a solvent, so as to prepare a key intermediate II; and (2) under protection of N2, dissolving the key intermediate II in an organic solvent, performing room-temperature reaction with 3,4-dihydropyran by taking an organic strong acid as a catalyst, so as to prepare a compound I shown in the specification, and n is equal to 1-5. The compounds are novel in structure, also synthesis steps are simple, yield is high, and production cost is low.
Design and synthesis of α-aryloxyphenylacetic acid derivatives: A novel class of PPARα/γ dual agonists with potent antihyperglycemic and lipid modulating activity
Shi, Guo Q.,Dropinski, James F.,McKeever, Brian M.,Xu, Shihua,Becker, Joseph W.,Berger, Joel P.,MacNaul, Karen L.,Eibrecht, Alex,Zhou, Gaochao,Doebber, Thomas W.,Wang, Peiran,Chao, Yu-Sheng,Forrest, Mike,Heck, James V.,Moller, David E.,Jones, A. Brian
, p. 4457 - 4468 (2007/10/03)
The synthesis and structure-activity relationships of novel series of α-aryloxyphenylacetic acids as PPARα/γ dual agonists are reported. The initial search for surrogates of the ester group in the screen lead led first to the optimization of a subseries w
Simple and efficient preparation of enantiopure alkyl α-hydroxyalkyl ketones
Ferrero,Galobardes,Martin,Montes,Romea,Rovira,Urpi,Vilarrasa
, p. 1608 - 1614 (2007/10/03)
The acylation reaction of organolithium reagents with pyrrolidine-derived α-benzyloxy and α-silyloxy carboxamides provides a simple and high-yielding method for the preparation of enantiopure α-benzyloxy and α-silyloxy ketones.
