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唐波,傅榕赓,李玲,谭桂林,张春桃.苯甲酰胺类磷酸二酯酶-4抑制剂的设计与合成[J].湖南中医药大学学报英文版,2016,36(3):27-29.[Click to copy
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| 苯甲酰胺类磷酸二酯酶-4抑制剂的设计与合成 |
| 唐波,傅榕赓,李玲,谭桂林,张春桃 |
| (湖南中医药大学药学院, 湖南 长沙 410208) |
| 摘要: |
| 目的 合成6个苯甲酰胺类磷酸二酯酶-4抑制剂。方法 以异香兰素为原料，经过成醚反应、氧化反应、Schotten-Baumann反应等制备目标化合物。结果 成功制备了6个目标化合物：Benzoic acid，4-[[3-（isobutoxy）-4-methoxybenzoyl]amino]（T1），Benzamide，4-[[3-（isobutoxy）-4-methoxybenzoyl]amino]（T2），Benzamide，4-（isobutoxy）-3-methoxy-N-[4-[[（1-methylethyl）amino]sulfonyl]phenyl]（T3），Benzoicacid，4-[[3-（cyclopentyloxy）-4-methoxybenzoyl]amino]（T4），Benzamide，4-[[3-（cyclopentyloxy）-4-methoxybenzoyl]amino]（T5），Benzamide，4-（cyclopentyloxy）-3-methoxy-N-[4-[[（1-methylethyl）amino]sulfonyl]phenyl]（T6），收率分别为66.7%、65.7%、18.4%、46.7%、76.8%和12.4%，其中化合物T1、T2、T3、T5、T6为新化合物。结论 所得产物的化学结构经1H-NMR、MS谱确证，与目标化合物相符。 |
| 关键词: 磷酸二酯酶-4抑制剂 苯甲酰胺类 设计与合成 |
| DOI：10.3969/j.issn.1674-070X.2016.03.008 |
| Received:October 29, 2015 |
| 基金项目:2013年湖南省教育厅资助研究生创新课题（CX2013B337）；湖南省教育厅药学特色专业资助。 |
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| Design and Synthesis of Benzamide Derivatives as Inhibitors of Phosphodiesterase-4 |
| TANG Bo,FU Ronggeng,LI Ling,TAN Guilin,ZHANG Chuntao |
| (Hunan University of Chinese Medicine, Changsha, Hunan 410208, China) |
| Abstract: |
| Objective To synthesize 6 phosphodiesterase-4 inhibitors of benzamide derivatives. Methods Isovanillin as the starting material, compounds was synthesized by etherification, oxidation reaction and Schotten-Baumann reaction. Results 6 target compounds were synthesized. Benzoic acid,4-[[3-(isobutoxy)-4-methoxybenzoyl]amino](T1), Benzamide,4-[[3-(isobutoxy)-4-methoxybenzoyl]amino](T2), Benzamide,4-(isobutoxy)-3-methoxy-N-[4-[[(1-methylethyl)amino]sulfonyl]phenyl] (T3), Benzoicacid, 4-[[3-(cyclopentyloxy)-4-methoxybenzoyl]amino](T4), Benzamide,4-[[3-(cyclopentyloxy)-4-methoxybenzoyl]amino](T5), Benzamide,4-(cyclopentyloxy)-3-methoxy-N-[4-[[(1-methylethyl)amino]sulfonyl]phenyl](T6). The yield were 66.7%, 65.7%, 18.4%, 46.7%, 76.8% and 12.4%, respectively. Conclution The structures of the target compounds were confirmed by 1H-NMR and MS methods. |
| Key words: PDE-4 inhibitors benzamide derivatives design and synthesis |
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