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那格列奈的合成工艺研究 被引量:4

Synthesis of Antidiabetic Drug Nateglinide
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摘要 以对异丙基环己基甲酸为原料,采用草酰氯进行氯化,合成对异丙基环己基甲酰氯,后与D-苯丙氨酸甲酯缩合制得那格列奈的工艺流程,通过对生产工艺参数(反应时间、温度、试剂选择等)和工艺流程进行分析、研究,优化工艺流程,使反应总收率提高到78%,且晶型转换完全。 Nateglinide is a kind of new antidiabetic drug, which has a wide market prospect. In view of the present problems in the synthesis of Nateglinide, the optimum synthesis conditions such as reaction time, temperature and reagent, etc were investigated and improved. Nateglinide was synthesized from trans-4-isopropylcyclo-hexane carboxlic acid as starting material,by used Oxalyl chloride chlorinated, which through alkalescence displacement and condensation and the total yield was 78%. And crystal transformation is not difficult. Such as more convenient and feasible operation, lower cost , higher yield, suitable for its industrialized production.
出处 《内蒙古石油化工》 CAS 2008年第23期19-20,共2页 Inner Mongolia Petrochemical Industry
关键词 那格列奈 工艺参数 合成 晶型转换 Nateglinide Production-technical Synthesized Crystal Transformation
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参考文献8

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二级参考文献8

  • 1Shinkai H, Nishikawa M, Sato Y, et al. N -(Cyclohexylcarbonyl) - D -Phenylalanines and Related Compounds. A New Class of Oral Hypo-glycemic Agents[J].J Med Chem , 1989, 32:1 436.
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  • 3Ajinomoto K K. Hypoglycemic agent [P]. EP: 0 196 222.1986-03-28.
  • 4Inagak I, Takashi, Hirakata-shi. Esomerization of 2- or 4-Substituted Cyclohex- anecarboxylic Acids to the Trans Iso-mers by Heating with Potassium Hydroxide [P]. EP:0 814 073, 1997-12-29.
  • 5Matsuzawa Tashihiro, Irie Yasuo. Preparation of Trans-4-isopropylcyclohexane - Carboxylic Acid Chloride [ P ]. JP:9 517 899, 1995-01-20.
  • 6Shigeshi Toyo shima, Yoshiko Seto, Kgi Toi. Preparation of D-Phenylalanine Derivatives and their Use as Hypo-glycemic A gents[P]. US: 4 816 484, 1989-03-28.
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