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Synthesis of novel thiol surrogate of Taxol: 2′-deoxy-2′-mercaptopaclitaxel |
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| Authors: | Xin Qi Sang-Hyeup Lee Yoon-Sik Lee |
| Affiliation: | a School of Chemical Engineering, Dalian University of Technology, Dalian 116012, People's Republic of China b School of Chemical Engineering, Seoul National University, Seoul 151-742, South Korea c Department of Chemistry, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Ku, Seoul 120-750, South Korea |
| Abstract: | Paclitaxel analogues with a thiol group in place of the hydroxyl group on the C-13 side chain constitute an interesting avenue of research for the study of new taxoid compounds. A synthetic route for the preparation of the exact thiol surrogate product of Taxol® by coupling (4S, 5S)-2,4-diphenyloxazoline-5-carboxylic acid with 7-triethylsilyl baccatin III, followed by ring-opening of the oxazoline intermediate with thiolacetic acid is described. |
| Keywords: | Taxol Mercaptopaclitaxel Oxazoline |
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