Optimization of the synthesis of photosensitizer purpurin-18 by orthogonal design
- Received Date: 2010-06-17
- Rev Recd Date: 2010-11-01
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Key words:
- medicinal chemistry /
- process improvement /
- purpurin-18 /
- orthogonal design /
- photosensitizer
Abstract: Objective To optimize the synthesis of photosensitizer purpurin-18(1). Methods Target compound 1 was synthesized through air oxidation and simultaneously ring cleavage of pheophorbide a (2) in presence of alkali. Four main factors influencing synthetic yield of 1 such as reaction time (A), concentration of potassium hydroxide (B), solvent (C) and weight ratio of material 2 to potassium hydroxide (D),which was chosed three levels respectively,were evaluated by the orthogonal experimental design of L9 (34). Results The optimization term of the synthesis of target compound 1 was B1C2A2D2. The yield of 1 was raised from 34.4% to 45.6%. Conclusion The yield was raised. The reaction time was shortened and the toxic solvent was removed. The procedure was suitable for industrial production.
Citation: | WANG Yao, YAO Jian-zhong, MIAO Zhen-yuan, SHENG Chun-quan, ZHANG Wan-nian. Optimization of the synthesis of photosensitizer purpurin-18 by orthogonal design[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(2): 114-116. |