Novel synthesis of isoxazoline indolizine amides for potential application to tropical diseases |
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| Authors: | Yong-Kang Zhang Jacob J Plattner Yasheen Zhou Musheng Xu Jianxin Cao Qingquan Wu |
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| Institution: | 1. Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA;2. WuXi AppTec (Tianjin) Co., Ltd, 111 Huanghai Road, 4th Avenue TEDA, Tianjin 300457, China;3. Shanghai ChemPartner, 998 Ha-lei Road, Zhangjiang High-tech Park, Pudong New Area, Shanghai 201203, China;4. Shanghai Medicilon, Inc., 585 Chuanda Road, Zhangjiang High-tech Park, Pudong New Area, Shanghai 201200, China |
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| Abstract: | Synthetically challenging isoxazoline indolizine amide compounds were designed and prepared for potential application to tropical diseases. Indolizine core structures were synthesized strategically as common intermediates for efficient derivatization. The chemistry for the syntheses of 8-(5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)indolizine-5-carboxamide (3) and 5-(5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-indolizine-8-carboxamide (4) is described in this Letter. |
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| Keywords: | Synthesis Isoxazoline Indolizine Parasiticide Tropical diseases |
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