首页> 外国专利> Derivative of 4,5-diaryl-3,4-dihydropyrimidine-2(1H)-thione, and a method for preparing a derivative of 4,5-diaryl-3,4-dihydropyrimidine-2(1H)-thione

Derivative of 4,5-diaryl-3,4-dihydropyrimidine-2(1H)-thione, and a method for preparing a derivative of 4,5-diaryl-3,4-dihydropyrimidine-2(1H)-thione

机译:4,5-二芳基-3,4-二氢嘧啶-2(1H)-硫酮的衍生物,以及制备4,5-二芳基-3,4-二氢嘧啶-2(1H)-硫酮的衍生物的方法

摘要

the subject invention is a phenolic derivative of 4,5 - diarylo - 3,4 - dihydropirymidyno - 2 (1h) - tionu, namely, 4 - (3 - hydroksyarylo) - 5 - arylo - 3,4 - dihydropirymidyno - 2 (1h) - mutation model and where the substituent y1, y2, y3,y4 means hydrogen atom or chlorine or fluorine or hydroxyl group, or a group alkilowu0105 c1 - c6 or alkoksylowu0105 c1 - c6 or aryloksylowu0105 or group alkenylowu0105 c1 - c6 or arylowa connected by one carbon atom or group arylowu0105 combined by two carbon atoms, comprising atoms zwiu0105zan e of y2 and y3 or y3 and y4 and substituent ar is formula iii, where x is carbon or nitrogen atom, z1, z2,z3 means hydrogen or fluorine atom atom or chlorine atom or group alkilowu0105 c1 - c6 or alkoksylowu0105 c1 - c6 or aryloksylowu0105 or group acyloksylowu0105 or c1 - c6 or arylowu0105 alkenylowu0105 group connected by one carbon atom or group arylowu0105 combined by two carbon atoms, including ato we associated with z1 and z2 z2 and z3 or a substituent r in the model and,hydrogen atom or group means alkilowu0105 c1 - c6 or ch2ar or ar, ar is formula iii where the substituent.the invention concerns the manufacture of 4,5 - also diarylo - 3,4 - dihydropiryrmdyno - 2 (1h) - tionu, which consists in combining tetrabutyloamoniowego fluoride (bu4nf) solution in the organic solvent containing 5 - arylo - 4 - (3 - alkilosililoksyarylo) - 3,4 - dihydropirymidyno - 2 (1h) - mutation of bs ploughing ii.the reaction results in water free conditions in an inert gas atmosphere at room temperature, after which the mixture are acidified, mixed at room temperature, then the mixture is extracted with solvent niemieszaju0105cym with water, and is washed with aqueous organic extracts solution the weak rules, separates the organic layer.and the water is removed by the addition of binding water, drained which oddestylowuje solvent, and the residue is purified by column chromatography. is 4 - (3 - hydroksyarylo) - 5 - arylo - 3,4 - dihydropirymidyno 2 (1h) - mutation model and which exhibits antiproliferative activity in relation to the action of tumour cells of human cancer.
机译:本发明是4,5-二芳基-3,4-二氢吡ry基-2(1h)-tionu的酚类衍生物,即4-(3-羟基己基)-5-芳基-3,4-二氢吡ry基-2(1h )-突变模型,其中的取代基y1,y2,y3,y4表示氢原子或氯或氟或羟基,或基团Alkilow u0105 c1-c6或alkoksylow u0105 c1-c6或芳基kylow u0105或alkenylowow 由一个碳原子连接的芳基或芳基或由两个碳原子结合的芳基基团,其包含y2和y3或y3和y4的原子zwi u0105zan e,且取代基ar为式iii,其中x为碳或氮原子,z1,z2,z3表示氢或氟原子或氯原子或烷基基团 u0105 c1-c6或alkoksylow u0105 c1-c6或芳基okylow u0105或基团acyloksylow u0105或c1-c6或arylow u0105链烯基 u0105由一个碳原子连接的基团或由两个碳原子结合的arylow u0105基团,包括与z1和z2,z2和z3相关联的ato或在模型中,氢原子或基团上的取代基r是指烷基或芳基,ar是式iii,其中取代基。本发明涉及4,5--二芳基-3,4-二氢吡咯烷基的制造-2(1h)-离子化,其方法是在含有5-芳基-4-(3-alkilosililoksyarylo)的有机溶剂中混合四丁基氟化铵(bu4nf)溶液-3,4-二氢吡喃基氨基-2(1h)-bs耕作突变ii。反应在室温下在惰性气体气氛中在无水条件下进行,然后将混合物酸化,在室温下混合,然后将混合物用溶剂niemieszaj萃取,并用含水有机萃取液洗涤溶解弱的规则,分离出有机层。通过加入结合水除去水,排干其中的奇异溶剂,并通过柱色谱法纯化残余物。是4-(3-Hydroksyarylo)-5-arylo-3,4-dihydropirymidyno 2(1h)-突变模型,它表现出与人类肿瘤细胞作用有关的抗增殖活性。

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