期刊文献+

乙酰基阿托品盐酸盐的制备 被引量:3

Preparation of Acetyl Atropine Hydrochloride
下载PDF
导出
摘要 乙酰基阿托品盐酸盐是合成硫酸阿托品的关键中间体,文章通过采用SO2Cl2-DMF组成的Vilsmeier-Haack型复合物作为脱水剂,以当量的乙酰托品酸和托品醇盐酸盐为原料,在室温下进行酯化反应制备乙酰基阿托品盐酸盐,收率接近定量。 Acetyl atropine hydrochloride is a key intermediates for the synthesis of atropine sulfate. N,N-dimethylchlorosulfitemethaniminium chloride (SO2CI2-DMF) was used in the synthesis of acety latropine hydrochloride via esterification between equimolar amounts of acetyl tropic acid and tropine hydrochloride under mild conditions with quantitative yield.
出处 《广东化工》 CAS 2013年第6期46-46,共1页 Guangdong Chemical Industry
关键词 Vilsmeier-Haack型复合物(SO2Cl2-DMF) 乙酰阿托品盐酸盐 酯化反应 中间体 N,N-dimethylchlorosulfltemethaniminiumchloride(SO2Cl2-DMF): acetylatropinehydrochloride: esterificationreaction: intermediate
  • 相关文献

参考文献5

  • 1杭州第一制药厂.硫酸阿托品的合成工艺[J].医药工业.1972,8:15-17.
  • 2刘娜,黄成军,周后元.氯化亚砜在有机合成中的应用[J].中国医药工业杂志,2007,38(3):156-163. 被引量:11
  • 3Kaul S, Kumar A, Sain B, et al. A simple and convenient one-pot synthesis of fatty acid esters from hindered alcohols using N , N-dimethylchlorosulfitemethaniminium chloride as dehydrating agent[J]. SynthCommun, 2002, 32(18): 2885-2891.
  • 4Urdaneta N A, Herrera J C, Salazar J, et al. Hydrochlorination of 2,3-acetylenic acids with thionyl chloride in dimethylformamide[J]. Synth Commun, 2002, 32(19): 3003-3009.
  • 5Arrieta A Aizpurua J M Palomo C. N,N-dimethylchlorosulfltemethaniminium chloride (SO2C12-DMF): a versatile dehydrating reagent[J]. Tetrahedron Lett, 1984, 25(31).. 3365 -3368.

二级参考文献30

  • 1Pizey SS.Synthetic Reagents[M].Vol 1,New York:John Wiley & Sons.Inc,1974:321-357.
  • 2Oka K.Some applications of thionyl chloride in synthetic organic chemistry[J].Synthesis,1981,(9):661-681.
  • 3Pearson AJ,Roush WR,et al.Handbook of reagents for organic synthesis activating agents and protecting groups[M].2nd ed,New York:John Wiley & Sons.Inc,2000:370-373.
  • 4Marcio CS,Antonio MS.Surface-mediated hydrohalogenation of isoprene.A facile preparation of prenyl halides[J].Synth Commun.2003,33(13):2181-2186.
  • 5Urdaneta NA,Herrera JC,Salazar J,et al.Hydrochlorination of 2.3-acetylenic acids with thionyl chloride in dimethylformamide[J].Synth Commun,2002,32(19):3003-3009.
  • 6Ghosh R,Chakraborty A,Maiti S.Highly stereoselective synthesis of peracylated α-aldopyranosyl chlorides from aldopyranose peracetates and thionyl chloride catalyzed by BiCl3 generated in situ from the procatalyst BiOC1[J].Tetrahedron Lett,2004,45:9631-9634.
  • 7Grimm JS,Maryanoff CA,Patel M,et al.Reaction safety:a critical parameter in the development of a scaleable synthesisof 2,3-bis-chloromethylpyridine hydrochloride[J].Org Process Res Dev,2002,6(6):938-942.
  • 8Taylor RE,Chen Y.Total synthesis of epothilones B and D[J].Org Lett,2001,3(14):2221-2224.
  • 9Gibson M,Goodman JM,Farrugia LJ,et al.Controlling neighbouring group participation from thioacetals[J].Tetrahedron Lett,2003,44:2841-2844.
  • 10Golubev AS,Pasternak PV,Shidlovskii AF,et al.Synthesis and some heterocyclisation reactions of CF2H-and CF2Cl-substituted 1,1-dicyanoethylenes[J].J Fluo Chem,2002,114(1):63-74.

共引文献10

同被引文献26

  • 1汪海波,陈佳辉.托品酸的制备[J].中国医药工业杂志,2004,35(11):645-645. 被引量:2
  • 2朱燕,张强,周玲,胡志力.拉呋替丁鼠伤寒沙门氏菌基因回复突变试验[J].齐鲁药事,2005,24(1):48-49. 被引量:1
  • 3王林,恽榴红,张其楷.胆碱能M受体拮抗剂:2α-(2',2'-二取代基-2'-羟基乙氧基)托品烷光学异构体合成[J].药学学报,1996,31(10):790-794. 被引量:3
  • 4Klomp D, Peters JA, Hanefeld U. Enzymatic kinetic reso- lution of tropic acid[J]. Tetrahedron: Asymmetry, 2005, 16 (23) : 3 892.
  • 5Long MT, Bartholomew BA, Smith M J, et al. Enzymolo- gy of oxidation of tropic acid to phenylacetic acid in me- tabolism of atropine by pseudomonas sp.strain AT3[J]. J Bacteriol, 1997,179(4) : 1 044.
  • 6Nagase T, Takahashi T, Sasaki T, et al. Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabi- cyclo [ 3.2. 1 ] octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors [ J ]. J Med Chem, 2009,52(14) :4111 -4114.
  • 7Gilbert A M, Stack G P, Nilakantan R, et al. Modu- lation of selective serotonin reuptake inhibitor and 5- HT1A antagonist activity in 8-aza-bicyclo [ 3.2.1 ] oc- tane derivatives of 2,3-dihydro-1,4-benzodioxane [ J ]. Bioorg Med Chem Lett,2004,14(2) :515 -518.
  • 8Yang Z H, Fang Y Y, Pham T A, et al. Synthesis and biological evaluation of 5-nitropyrimidine analogs with azabicyclic substituents as GPR119 agonists [ J ]. Bioorg Med Chem Lett,2013,23(5) :1519 -1521.
  • 9MeClure K F, Darout E, Guimar~es C R, et al. Acti- vation of the G-protein coupled receptor 119:A confor- mation-based hypothesis for understanding agonist re- sponses[ J]. J Med Chem,2011,54(6) :1948.
  • 10Pham T A, Yang Z H, Fang Y Y, et al. Synthesis and biological evaluation of novel 2, 4-disubstituted quinazoline analogues as GPR119 agonists [ J ]. Bioorg Med Chem ,2013,21 (5) : 1349 - 1356.

引证文献3

二级引证文献3

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