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Volume 30 Issue 4
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2012  >  30(4): 287-288,304

ZHAO Ming-zhu, ZANG Cheng-xu, CAI Zhan, JIANG Zhi-hui, HUANG Jing-hua, ZHANG Da-zhi. Process improvement of tamibarotene preparation[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(4): 287-288,304.
Citation: ZHAO Ming-zhu, ZANG Cheng-xu, CAI Zhan, JIANG Zhi-hui, HUANG Jing-hua, ZHANG Da-zhi. Process improvement of tamibarotene preparation[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(4): 287-288,304.
shu

Process improvement of tamibarotene preparation

  • 1.

    Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • 2.

    Guilin Eight Plus One Pharmaceutical Co., Ltd., Gui Lin 541004, China

  • Received Date: 2011-09-28
  • Rev Recd Date: 2012-01-11
  • Objective To improve the preparation process of tamibarotene.Methods 1,2,3,4-tetrahydro-1,1,4,4-tetram-ethyl-6-acelylaminonaphthalimide was prepared from 2,5-dimethyl-2,5-hexanediol by chloridized and Friedel-Craft reaction with acetauilide,which was subjected to deacylation, acylation and hydrolyzation to give tamibarotene.Results The process was successfully improved due to low cost,easier post-processing and good yield. The purity of the product was high (>99.7%) and no impurity more than 0.1%. Conclusion The total yield of the improved process was 26.6%. which was more suitable for industrial manufacturing.the structure of temibarotene was confirmed by 1H-NMR,ESl-MS and elementary analysis.
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  • 1. 

    沈阳化工大学材料科学与工程学院 沈阳 110142

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Process improvement of tamibarotene preparation

  • 1. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • 2. Guilin Eight Plus One Pharmaceutical Co., Ltd., Gui Lin 541004, China
  • Received Date: 2011-09-28
  • Rev Recd Date: 2012-01-11

Abstract: Objective To improve the preparation process of tamibarotene.Methods 1,2,3,4-tetrahydro-1,1,4,4-tetram-ethyl-6-acelylaminonaphthalimide was prepared from 2,5-dimethyl-2,5-hexanediol by chloridized and Friedel-Craft reaction with acetauilide,which was subjected to deacylation, acylation and hydrolyzation to give tamibarotene.Results The process was successfully improved due to low cost,easier post-processing and good yield. The purity of the product was high (>99.7%) and no impurity more than 0.1%. Conclusion The total yield of the improved process was 26.6%. which was more suitable for industrial manufacturing.the structure of temibarotene was confirmed by 1H-NMR,ESl-MS and elementary analysis.

ZHAO Ming-zhu, ZANG Cheng-xu, CAI Zhan, JIANG Zhi-hui, HUANG Jing-hua, ZHANG Da-zhi. Process improvement of tamibarotene preparation[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(4): 287-288,304.
Citation: ZHAO Ming-zhu, ZANG Cheng-xu, CAI Zhan, JIANG Zhi-hui, HUANG Jing-hua, ZHANG Da-zhi. Process improvement of tamibarotene preparation[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(4): 287-288,304.
shu

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