SHAN Bin, SUN Miao, MENG Zhi, HAN Guiyan, QIAN Qihan, LIU Minghui, YAO Jianzhong. Optimization of synthesis of photosensitizer chlorin e6-C15 monomethyl ester by the orthogonal design[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(2): 122-124. doi: 10.3969/j.issn.1006-0111.2015.02.007
| Citation:
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SHAN Bin, SUN Miao, MENG Zhi, HAN Guiyan, QIAN Qihan, LIU Minghui, YAO Jianzhong. Optimization of synthesis of photosensitizer chlorin e6-C15 monomethyl ester by the orthogonal design[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(2): 122-124. doi: 10.3969/j.issn.1006-0111.2015.02.007
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Optimization of synthesis of photosensitizer chlorin e6-C15 monomethyl ester by the orthogonal design
- 1.
Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, China
- 2.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China
- 3.
Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, China;School of Pharmacy, Second Military Medical University, Shanghai 200433, China
- Received Date: 2014-08-26
- Rev Recd Date:
2014-11-17
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Abstract
Objective To optimize the synthesis of photosensitizer chlorine e6-C15 monomethyl ester (1). Methods Target compound 1 was synthesized through E ring cracking of pheophorbide a (3) in methanol solution of potassium hydroxide followed by adding H2O for ester hydrolysis with "one-pot" process. Four main factors that influencing the synthetic yield of target compound 1 are ring cleavage reaction time (A), reflux hydrolysis reaction time (B), alkali concentration (C) and weight ratio of material 3 to alkali (D). Each of the four factors was chosen at three levels and evaluated by the orthogonal experimental design of L9 (34). Results The optimization terms of the synthesis of target compound 1 were B1C2A2D1. The yield of compound 1 was raised from 43.0% to 56.5%. Conclusion The developed process has the advantages of simple operation, good safety and high reaction yield, and is suitable for industrial production.
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