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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.
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.
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.
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