B-SBA-5催化分解联苯类α-氨基膦酸酯化合物及其抗病毒活性研究.pdfVIP

B-SBA-15 催化合成联苯类α-氨基膦酸酯化合物及其抗病毒活性研究 摘要 B-SBA-15 催化合成联苯类α-氨基膦酸酯化合物及其抗 病毒活性研究 摘要：鉴于传统催化剂的造价高、不能循环使用的缺点，本文将活性组分硼原子负 载在介孔材料中，制备可循环使用的 B-SBA-15 催化剂；并应用于联苯类 α-氨基膦 酸酯的合成中，取得较好的循环效果；本文以抗病毒药剂氨基膦酸酯类化合物为先 导化合物，通过Suzuki 反应与Mannich 反应合成联苯类α-氨基膦酸酯衍生物，且目 1 13 31 标化合物结构均通过 HNMR ， CNMR ， PNMR ，IR ，HRMS 和元素分析确证，对 所合成的目标化合物进行了生物活性研究，发现联苯类 α-氨基膦酸酯化合物具有较 好的抗TMV 和抗CMV 活性，其中4d 化合物在500 µg/mL 浓度下对烟草花叶病毒 (TMV) 的防效达到了64%，化合物4s 在500 µg/mL 浓度下对黄瓜花叶病毒（CMV) 的防效达到了 79.8%，远高于对照药剂宁南霉素(对 TMV 和 CMV 的防效分别为 55.4%和 53.2%)。该类化合物对植物病毒具有很好的抗病毒活性，可应用于抗植物 病毒农药的制备，尤其是抗黄瓜花叶病毒（CMV ）农药。 关键词：ɑ-氨基膦酸酯、联苯类、活性基团、生物活性 I B-SBA-15 催化合成联苯类α-氨基膦酸酯化合物及其抗病毒活性研究 摘要 The synthesis of biphenyl derivatives of α-aminophosphonates compounds catalyzed by B-SBA-15 and its antiviral activity Abstract: In view of the shortcoming of traditional catalyst, we conceive loading the active component boron into mesoporous materials to prepare the recycled catalyst B-SBA-15. It was applied to the synthesis of the biphenyl derivatives of α-aminophosphonates and proved circulating effectively. Then using α-aminophosphonate as leading compound, the biphenyl α-aminophosphonates derivatives was synthesized via two step involving Suzuki reaction and Mannich reaction. And the target compounds were firstly synthesized. All compounds were confirmed by 1HNMR, 13CNMR, 31PNMR, IR, HRMS and elemental analysis. The results of bioassay showed that the biphenyl derivatives of α-aminophosphonates exhibited certain anti-TMV and anti-CMV respectively. Compound 4d exhibited higher activity (64%) on anti-TMV in 500 μg/mL than Ningnanmycin (55.4%), and compound 4s exhibited