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WU Junqi, YE Xiaofei, HUANG Lei, CHAI Xiaoyun, JIN Yongsheng, YU Shichong. Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 171-173. doi: 10.3969/j.issn.1006-0111.2016.02.018
Citation: WU Junqi, YE Xiaofei, HUANG Lei, CHAI Xiaoyun, JIN Yongsheng, YU Shichong. Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 171-173. doi: 10.3969/j.issn.1006-0111.2016.02.018

Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates

doi: 10.3969/j.issn.1006-0111.2016.02.018
  • Received Date: 2015-11-20
  • Rev Recd Date: 2015-12-30
  • Objective To optimize novel triazole antifungal compounds synthesis of key intermediates. Methods The orthogonal experimental design is used, emphasizing on four factors including the reaction temperature, the weight ratio of material, reaction time and solvent on the yield. Results The effect of reaction temperature on the reaction yield is the most significant, followed by reaction time; the weight ratio of material and solvent on the yield impact is not obvious. Conclusion The new technology has several advantages and yields up to about 50%, less reactive impurities, easy post processing.
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    [6] Ichikawa T, Yamada M, Yamaguchi M, et al. Optically active antifungal azoles. XⅢ. Synthesis of Stereoisomers and Metabolites of 1-[(1R, 2R)-2-(2, 4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1, 2, 4-triazol-1-yl) propyl]-3-[4-(1H-1-tetrazolyl) phenyl]-2-imidazolidinone(TAK-456)[J]. Chemic Pharmaceut Bull, 2001, 49(9):1110-1119.
    [7] Cao X, Sun Z, Cao Y, et al. Design, synthesis, and structure activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility[J]. J Med Chem, 2014, 57(9):3687-3706.
    [8] 梁文杰,钟宏,何谋海. 乙氧基羰基异硫氰酸酯的合成工艺[J]. 化工进展,2011, 30(S1):610-612.
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Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates

doi: 10.3969/j.issn.1006-0111.2016.02.018

Abstract: Objective To optimize novel triazole antifungal compounds synthesis of key intermediates. Methods The orthogonal experimental design is used, emphasizing on four factors including the reaction temperature, the weight ratio of material, reaction time and solvent on the yield. Results The effect of reaction temperature on the reaction yield is the most significant, followed by reaction time; the weight ratio of material and solvent on the yield impact is not obvious. Conclusion The new technology has several advantages and yields up to about 50%, less reactive impurities, easy post processing.

WU Junqi, YE Xiaofei, HUANG Lei, CHAI Xiaoyun, JIN Yongsheng, YU Shichong. Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 171-173. doi: 10.3969/j.issn.1006-0111.2016.02.018
Citation: WU Junqi, YE Xiaofei, HUANG Lei, CHAI Xiaoyun, JIN Yongsheng, YU Shichong. Orthogonal design optimization in synthesis of novel triazole antifungal compounds as key intermediates[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 171-173. doi: 10.3969/j.issn.1006-0111.2016.02.018
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