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4-苄基-2-羟基-吗啉-3-酮的合成 被引量:1

Synthesis of 4-benzyl-2-hydroxy-1,4-oxazin-3-one
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摘要 以乙醛酸和N-苄基乙醇胺为原料,合成4-苄基-2-羟基-吗啉-3-酮。通过正交实验考察了反应条件对目标产物收率的影响。结果表明,当原料摩尔比n(乙醛酸)∶n(N-苄基乙醇胺)=2∶1,反应时间22 h,反应溶剂四氢呋喃用量35 mL,反应温度65℃时,目标产物的收率最高可达62%。并进一步考察了反应温度和原料摩尔比对反应收率的影响。 4-Benzyl-2-hydroxy-1,4-oxazin-3-one could be synthesized from glyoxylic acid and N-benzylethanolamine. The effect of reaction condition on yield were researched by orthogonal experiment,the optimum condition were as follows:mole ratio of glyoxylic acid to N-benzylethanolamine 2 : 1, reaction time 26 h,THF 35 mL, temperature 65 ℃. Under these conditions, the product yield was 62%. And to further study influence of the temperature and molar ratio on the reaction yield.
出处 《应用化工》 CAS CSCD 2008年第12期1484-1485,1499,共3页 Applied Chemical Industry
关键词 4-苄基-2-羟基-吗啉-3-酮 合成 阿瑞吡坦 N-苄基乙醇胺 4-benzyl-2-hydroxy-1,4-oxazin-3-one synthesis aprepitant N-benzylethanolamine
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  • 1Patel L, Lindley C. Aprepitant-a novel NK1-receptor antagonist [ J ]. Expert Opin Pharmacother, 2003,4: 2279- 2296. 被引量:1
  • 2Pendergrass K, Hargreaves R, Petty K J, et al. Aprepitant : an oral NK1 antagonist for the prevention of nausea and vomiting induced by highly emetogenic chemotherapy [ J ]. Drags Today(Barc) ,2004,40 : 853-863. 被引量:1
  • 3De Jonge M E, Huitema A D, Holtkamp M J, et al. Aprepitant inhibits cyclophosphamide bioactivation and thiotepa metabolism [ J ]. Cancer Chemother Pharmacol, 2005,56 : 370-378. 被引量:1
  • 4Warr D G, Gruuberg S M, Gralla R J, et al. The oral NK( 1 ) antagonist aprepitant for the prevention of acute and delayed chemotherapy-induced nausea and vomiting: Pooled data from 2 randomised, double-blind, placebo controlled trials [ J]. Eur J Cancer,2005,41 : 1278-1285. 被引量:1
  • 5Todd D Nelson, Jonathan D Rosen, Karel M J Brands, et al. Syntheses of morpholine-2,3-dionesand 2-hydroxymorpholin-3-ones :intermediates in the synthesis of aprepitant [ J ]. Tetrahedron Letters ,2004,45:8917-8920. 被引量:1
  • 6Louis S Crocker,Belle Mead,Karel M J Brands,et al. 4- Benzyl-2-hydroxy-1,4-oxazine-3-one and polymorphic forms : US,6538134B2 [ P]. 2003-03-25. 被引量:1
  • 7Torosyan S O, Nazaretyan A K, Karapetyan L P, et al. Alkylation of ethanolamine by alkyl halides in alkaline aqueous solutions in the presence of catamine AB [ J ]. Trudy Erevanskogo Zooveterinarnogo Instituta, 1982,53: 113-117. 被引量:1

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