| 4-氨基-4-甲基哌啶二对甲苯磺酸盐的合成 |
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| 引用本文： | 谭红梅,马玉卓.4-氨基-4-甲基哌啶二对甲苯磺酸盐的合成[J].广东药学院学报,2011,27(3):247-249. |
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| 作者姓名： | 谭红梅 马玉卓 |
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| 作者单位： | 广东药学院药科学院,广东广州,510006 |
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| 摘 要： | 目的 合成二肽基肽酶4抑制剂ABT-279和K-579的重要中间体4-氨基4-甲基哌啶二对甲苯磺酸盐.方法 以4-哌啶甲酸乙酯为原料,经N-Boc保护、烷基化、酰胺化、Hofmann降解和N-Boc脱保护5步反应,制备得4-氨基4-甲基哌啶二对甲苯磺酸盐.结果 4-哌啶甲酸乙酯为原料合成目标化合物的总收率为49.5%....
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| 关 键 词： | 4-氨基-4-甲基哌啶二对甲苯磺酸盐 二肽基肽酶4抑制剂 4-哌啶甲酸乙酯 |
Synthesis of 4-amino-4-methylpiperidine di-p-toluenesulfonate |
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| TAN Hong-mei,MA Yu-zhuo.Synthesis of 4-amino-4-methylpiperidine di-p-toluenesulfonate[J].Academic Journal of Guangdong College of Pharmacy,2011,27(3):247-249. |
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| Authors: | TAN Hong-mei MA Yu-zhuo |
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| Institution: | (School of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China) |
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| Abstract: | Objective To synthesize the key intermediate 4-amino-4-methylpiperidine di-p-toluenesulfonate of ABT-279 and K-579,which are potential dipeptidyl peptidase-4 inhibitors.Methods The key intermediate was prepared starting from ethyl piperidine-4-carboxylate via N-Boc protection,alkylation,amidation,Hofmann rearrangement and N-Boc deprotection.Results The overall yield of process was 49.5%.Conclusion This synthetic process is suitable for large scale preparation with a higher yield,lower cost and simplified operation. |
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| Keywords: | 4-amino-4-methylpiperidine di-p-toluenesulfonate 4-amino-4-methylpiperidinedi-p-toluenesulfonate piperidine-4 -carboxylate |
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