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甲磺酸加贝酯的合成 被引量：4

Synthesis of Gabexate Mesylate
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摘要 6-氨基己酸与S-甲基异硫脲硫酸盐反应后盐酸化得6-胍基己酸盐酸盐,与由对羟基苯甲酸乙酯经氯化亚砜缩合得到的4,4’-(亚硫酰二氧基)二苯甲酸二乙酯反应,得到胰腺炎治疗药物甲磺酸加贝酯,总收率约为63%。 Gabexate mesylate was synthesized from 6-aminohexanoic acid and S-methylisothiourea sulfate by condensation to give 6-guanidohexanoic acid, which was subjected to reaction with 4,4＇- [sulfinylbis （oxy） ] bisbenzoic acid diethyl ester followed by mesylate salt formation with an overall yield of about 63 %.
作者 陆修涛 杨文革 胡永红 赵聪
机构地区 南京工业大学制药与生命科学学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2007年第11期753-754,共2页 Chinese Journal of Pharmaceuticals
关键词 甲磺酸加贝酯 胰腺炎 合成 gabexate mesilate pancreatitis synthesis
分类号 R979.9 [医药卫生—药品]
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参考文献8

  • 1蒋伯诚.丝氨酸蛋白分解酶抑制剂[J].药学进展,1991,15(3):139-142. 被引量：5
  • 2彭国林,李兆申.加贝酯防治急性胰腺炎应用现状[J].胰腺病学,2005,5(3):177-179. 被引量：15
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二级参考文献20

  • 1吴叔明,徐华,戈之铮,莫剑忠,陈胜良,杨川华.加贝酯对Oddi括约肌运动的影响[J].中华消化杂志,2004,24(8):464-467. 被引量：26
  • 2Buchler M, Malfertheiner P, Uhl W, et al. Gabexate mesilate in human acute pancreatitis. German pancreatitis study group. Gastroenterology, 1993, 104:1165-1170.
  • 3Andriulli A, Leandro G, Clemente R, et al. Meta-analysis of somatostatin, octreotide and gabexate mesilate in the therapy of acute pancreatitis. Aliment Pharmacol Ther, 1998, 12:237-245.
  • 4Seta T, Noguchi Y, Shimada T, et al. Treatment of acute pancreatitis with protease inhibitors: a meta-analysis. Eur J Gastroenterol Hepatol, 2004, 16:1287-1293.
  • 5Pelagotti F, Cecchi M, Messori A, et al. Use of gabexate mesylate in Italian hospitals: a multicentre observational study. J Clin Pharm Ther, 2003, 28:191-196.
  • 6Chen HM, Chen JC, Hwang TL, et al. Prospective and randomized study of gabexate mesilate for the treatment of severe acute pancreatitis with organ dysfunction. Hepatogastroenterology, 2000, 47:1147-1150.
  • 7Yang CY, Chang-Chien CS, Liaw YF. Controlled trial of protease inhibitor gabexelate mesilate (FOY) in the treatment of acute pancreatitis. Pancreas, 1987, 2:698-700.
  • 8Valderrama R, Perez-Mateo M, Navarro S, et al. Multicenter double-blind trial of gabexate mesylate (FOY) in unselected patients with acute pancreatitis. Digestion, 1992, 51:65-70.
  • 9Harada H, Miyake H, Ochi K, et al. Clinical trial with a protease inhibitor gabexate mesilate in acute pancreatitis. Int J Pancreatol, 1991, 9:75-79.
  • 10Pezzilli R, Miglioli M. Multicentre comparative study of two schedules of gabexate mesilate in the treatment of acute pancreatitis. Italian Acute Pancreatitis Study Group. Dig Liver Dis, 2001, 33:49-57.

共引文献19

同被引文献31

引证文献4

二级引证文献11

中国医药工业杂志
2007年 第11期

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