中华医学超声杂志

应用化学 ›› 1998, Vol. 0 ›› Issue (4): 98-100.

• 研究论文 • 上一篇    下一篇

维生素K1合成的改进

冀亚飞1, 张雁秋1, 石俊英2   

  1. 1. 中国矿业大学能源化工系 徐州 221008;
    2. 华东理工大学精细化工研究所 上海
  • 收稿日期:1997-10-09 修回日期:1997-12-25 出版日期:1998-08-10 发布日期:1998-08-10

Improvement in Vitamin K1 Synthesis

Ji Yafei1, Zhang Yanqiu1, Shi Junying2   

  1. 1. Department of Energy Utilization and Chemical Engineering, ChinaUniversity of Mining and Technology, Xuzhou 221008;
    2. Research Institute of Fine Chemicals, East China Universityof Science and Technology, Shanghai
  • Received:1997-10-09 Revised:1997-12-25 Published:1998-08-10 Online:1998-08-10

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摘要： 维生素K1分子侧链上有一双键,因而存在几何异构体.天然维生素K1是2,3-反式构型,合成品为顺式和反式异构体的混合物,而顺式异构体几乎没有生理活性.故此,八十年代以后,各国药典均对维生素K1顺式异构体规定了限量,中国药典(1995版)规定顺式异构体的含 量不得超过21.0%[1].目前国内流行的制备方法是以甲萘醌为起始原料,须经还原、乙酰化、水解、缩合、再水解和氧化五步反应制得[2],步骤长、收率低、对环境污染大.而用异植物醇合成引入侧链时,制备的维生素K1顺式异构体含量较高,达不到药典要求.为满足新版药典的规定,需使用昂贵的天然植物醇.

关键词: 维生素K1, 合成, 植基氯, 植基溴

Abstract: The Ruettimnann's method[5] for vitamin K1 synthesis has been improved by usingphase transfer catalyst in Diels-Alder condensation and using mixed trans-cis phytyl chlorideinstead of natural phytol as starting material in the synthesis.The vitamin K1 then obtainedby a retro-Diels-Alder reaction has a cis-trans isomer ratio of 20.35 to 79.65 which meets theChinese pharmacopia standard.Phytyl bromide in this case gave vitamin K1 with cis-trans ratio of 26.30 to 73.70.

Key words: vitamin K1, synthesis, phytyl chloride, phytyl bromide

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