以自制2-氨基-4-甲基-5-（1H-1,2,4-三唑-1-基）-噻吩-3-甲酸乙酯为起始原料制得膦亚胺,膦亚胺与苯基异氰酸酯作用得到碳二亚胺,在碳酸钾的催化下,碳二亚胺与酚反应得到4个新型的2-芳氧基-3-苯基-5-甲基-6-（1H-1,2,4-三唑-1-基）噻吩并...以自制2-氨基-4-甲基-5-（1H-1,2,4-三唑-1-基）-噻吩-3-甲酸乙酯为起始原料制得膦亚胺,膦亚胺与苯基异氰酸酯作用得到碳二亚胺,在碳酸钾的催化下,碳二亚胺与酚反应得到4个新型的2-芳氧基-3-苯基-5-甲基-6-（1H-1,2,4-三唑-1-基）噻吩并[2,3-d]嘧啶-4（3H）-酮衍生物（3a-3d）,收率为70%~86%,通过1 H NMR、MS和元素分析等方法对合成化合物进行了结构表征,并初步测定了合成化合物的生物活性。结果表明,目标化合物对常见农作物部分菌体均表现出一定的抑菌活性,其中以2-萘氧基-3-苯基-5-甲基-6-（1H-1,2,4-三唑-1-基）噻吩并[2,3-d]嘧啶-4（3H）-酮活性最好,在浓度为5×10-5g/L时,对苹果轮纹菌的抑制率达到80%。展开更多
A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characteriz...A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.展开更多
以硫脲和氯乙酸为原料,在无溶剂和350 W微波辐射4 m in条件下,缩合生成中间体2,4-噻唑烷二酮(Ⅰ)产率91.5%;随后在无溶剂和400 W微波辐射5 m in条件下,通过V ilsm e ier甲酰化反应,生成中间体4-氯-5-甲酰基噻唑-2(3H)-酮(Ⅱ),产率86.7%...以硫脲和氯乙酸为原料,在无溶剂和350 W微波辐射4 m in条件下,缩合生成中间体2,4-噻唑烷二酮(Ⅰ)产率91.5%;随后在无溶剂和400 W微波辐射5 m in条件下,通过V ilsm e ier甲酰化反应,生成中间体4-氯-5-甲酰基噻唑-2(3H)-酮(Ⅱ),产率86.7%;最后以正丙醇为溶剂,450 W微波辐射7 m in条件下,成环得到5-氨基-噻唑[4,5-d]嘧啶-2(3H)-酮(Ⅲ),产率80.5%。反应总产率为63.9%。合成产物与中间体的结构经1HNMR,MS和元素分析确认。展开更多
文摘以自制2-氨基-4-甲基-5-（1H-1,2,4-三唑-1-基）-噻吩-3-甲酸乙酯为起始原料制得膦亚胺,膦亚胺与苯基异氰酸酯作用得到碳二亚胺,在碳酸钾的催化下,碳二亚胺与酚反应得到4个新型的2-芳氧基-3-苯基-5-甲基-6-（1H-1,2,4-三唑-1-基）噻吩并[2,3-d]嘧啶-4（3H）-酮衍生物（3a-3d）,收率为70%~86%,通过1 H NMR、MS和元素分析等方法对合成化合物进行了结构表征,并初步测定了合成化合物的生物活性。结果表明,目标化合物对常见农作物部分菌体均表现出一定的抑菌活性,其中以2-萘氧基-3-苯基-5-甲基-6-（1H-1,2,4-三唑-1-基）噻吩并[2,3-d]嘧啶-4（3H）-酮活性最好,在浓度为5×10-5g/L时,对苹果轮纹菌的抑制率达到80%。
文摘A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells.
文摘以硫脲和氯乙酸为原料,在无溶剂和350 W微波辐射4 m in条件下,缩合生成中间体2,4-噻唑烷二酮(Ⅰ)产率91.5%;随后在无溶剂和400 W微波辐射5 m in条件下,通过V ilsm e ier甲酰化反应,生成中间体4-氯-5-甲酰基噻唑-2(3H)-酮(Ⅱ),产率86.7%;最后以正丙醇为溶剂,450 W微波辐射7 m in条件下,成环得到5-氨基-噻唑[4,5-d]嘧啶-2(3H)-酮(Ⅲ),产率80.5%。反应总产率为63.9%。合成产物与中间体的结构经1HNMR,MS和元素分析确认。
