期刊文献+

四氢萘类化合物合成工艺研究 被引量:1

Synthesis of substituted tetrahydronaphthalene
下载PDF
导出
摘要 目的优化取代四氢萘类化合物的合成工艺,重点考察10%Pd/C对关键中间体合成的影响。方法平行试验比较10%Pd/C和三乙基硅烷催化羰基还原反应,并对实验结果进行总体分析;对10%Pd/C催化还原采用正交设计法,考察反应物与10%Pd/C的投料比例及溶剂对收率的影响。结果 10%Pd/C催化羰基还原的成本明显低于三乙基硅烷,且收率高,杂质少,易处理;正交试验证实,催化剂与反应物的投料比例对反应的影响最为显著。结论实验证实,利用10%Pd/C催化还原关键中间体,使得取代四氢萘类化合物的合成路线更加符合工业生产的要求。 Objective To optimize the synthesis of substituted tetrahydronaphthalene and investigate the influence of 10% Pd/C catalyst in the synthesis of key intermediate. Methods A parallel test was carried out to compare the catalytic activity of triethyl silicane and the 10% Pd/C catalyst, including the total analysis of experimental result . And orthogonal experimental design was used and the influence of solvent and reactant ratio on the yield were investigated. Results The cost of the 10% Pd/C eatalyst was obvious- ly lower than that of triethyl silieane,with high yield, little impurity easy effluent disposal. Orthogonal test confirms that the ratio of re- actant and catalystthe was the most significant factor. Conclusion The experiments proved that the optimal preparation procedure was much more available for industrial production using the 10% Pd/C as a catalyst.
出处 《药学实践杂志》 CAS 2012年第1期35-37,共3页 Journal of Pharmaceutical Practice
基金 国家自然科学基金(20972187)
关键词 取代四氢萘 合成 正交设计 substituted tetrahydronaphthalene synthesis orthogonal design
  • 相关文献

参考文献6

  • 1周有骏,姚斌,朱驹.具有抗真菌活性的N-取代-2-氨基-1,2,3,4-四氢萘化合物及其盐类:中国,1817851A[P].2006-10-24.
  • 2Paull KD,Zee-Cheng RK,Cheng CC.Some substituted naphthazarins as potential anticancer agents[J].J Med Chem,1976,19(2):337.
  • 3Hamdy NA,Gamal-Eldeen AM,Abdel-Aziz HA,et al.Modulation of carcinogen metabolizing enzymes by new fused heterocycles pendant to 5,6,7,8-tetrahydronaphthalene derivatives[J].Eur J Med Chem,2010,45(2):463.
  • 4Varella MH,de Mello FG,Linden R.Evidence for an antiapoptotic role of dopamine in developing retinal tissue[J].J Neurochem,1999,73(2):485.
  • 5Hui Tang You Jun Zhou Yao Wu Li Jia Guo Lv Can Hui Zheng Jun Chen Ju Zhu.Design,synthesis and antifungal activities in vitro of novel tetralin compounds[J].Chinese Chemical Letters,2008,19(3):264-268. 被引量:2
  • 6Norlander JE,Payne MJ,Njoroge FG,et al.A short enantiospecific synthesis of 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN)[J].J Org Chem,1985,50,3619.

二级参考文献14

  • 1H. Vanden Bossche, L. Koymans, Mycoses 41 (1998) 32.
  • 2P. Kale, L.B. Johnson, Drug Today (Barc) 41 (2005) 91.
  • 3D.J. Sheehan, C.A. Hitchcock, C.M. Sibley, Clin. Microbiol. Rev. 12 (1999) 40.
  • 4H. Wulff, M.J. Miller, W. Hansel, S. Grissmer, M.D. Cahalan, K.G. Chandy, Proc. Natl. Acad. 97 (2000) 8151
  • 5J.E Rogers, A.N. Nafziger, J.S. Bertino, Am. J. Med. 113 (2002) 746.
  • 6F.W. Su, P. Perumalswami, L.C. Grammer, Allergy 58 (2003) 1215.
  • 7M.R. Jeng, J. Feusner, Pediatr Hematol. Oncol. 18 (2001) 137.
  • 8M. Aslam, J. Aslam, J. Clin. Gastroenterol. 33 (2001) 407.
  • 9H.T. Ji, W.N. Zhang, Y.J. Zhou, et al. J. Med. Chem. 43 (2000) 2493.
  • 10H.T. Ji, W.N. Zhang, M. Zhang, et al. J. Med. Chem. 46 (2003) 474.

共引文献2

同被引文献12

  • 1刘刚,李晓燕.喹唑啉类化合物生物活性研究进展[J].药学进展,2007,31(12):542-550. 被引量:10
  • 2Chandrika P M,Yakaiah T,Gayatri G,et al. Click chemistry: studies on the synthesis of novel fluorous tagged triazo1-4 -yl substituted quinazoline derivatives and their biological evalua- tion-theoretical and experimental validation[J]. Eur J Med Chem,2010,45 : 78-84.
  • 3E1-Gazzar ABA, Youssef MM, Youssef AM S, et al. Design and synthesis of azolopyrimidoquinolines, pyrimidoquinazo- lines as anti-oxidant, anti-inflammatory and analgesic activi- ties[J]. Eur J Med Chem, 2009,44 ~ 609-624.
  • 4Lee J Y, Park YK, Seo SH, et al. 1,4-dioxane-fused 4-anilino- quinazoline as inhibitors of epidermal growth factor receptor kinase[J]. Arch Pharm Res,2001, 334(11) :357-360.
  • 5Lee JY, f.ee YS, Park HK, et al. 4-(Phenylamino) [1, 41 dioxano~2,3-g~ quinazoline derivatives and process for pre- paring the same: USA,2003045537[P]. 2003-03-06.
  • 6Ioannis K, Abdelhakim E, Elisabeth S, et al. Rapid synthesis of 2, 3-disubstituted-quinazolin-4-ones enhanced by micro- wave-assisted decomposition of formamide [J]. Tetrahedron Lett,2007, 48: 6609.
  • 7NCCLS. Reference method for broth dilution antifungal sus- ceptibility testing of yeasts~ approved standard ES~. 2nd ed, Villanova : [s. n. ], 2000.
  • 8李文举,欧阳贵平,张广龙.4-取代氨基喹唑啉类化合物的研究进展[J].精细化工中间体,2009,39(3):15-20. 被引量:3
  • 9宋桂红,张珏,张晓梦,宁微微,纪亚忠,惠宁,赵亚南,周有骏,朱驹,吕加国.南德士抑制人精子顶体酶活性的实验研究[J].中华男科学杂志,2009,15(8):700-702. 被引量:4
  • 10宁微微,刘雪飞,张晓梦,郑灿辉,盛春泉,周有骏,章玲,吕加国,朱驹.新型喹唑啉酮类先导物的设计、合成及抑制人顶体酶活性研究[J].药学实践杂志,2010,28(4):296-298. 被引量:3

引证文献1

二级引证文献1

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部