乙酰乙酸乙酯置于溴体系中,用 乙醚,乙醇 作为反应溶剂,化学反应 4.0H,反应生成 2-氨基-4-噻唑乙酸乙酯 参考文献:用于组装 Hiv-1 Tar Rna 结合配体的靶向叠氮-炔环加成. 标题:用于组装 Hiv-1 Tar Rna 结合配体的靶向叠氮-炔环加成. 摘要:高度保守的 Hiv-1 反式激活反应元件 (Tar) 与反式激活蛋白 Tat 结合,并促进潜伏状态下的病毒复制.通过选择性靶向 Tar Rna 来抑制 Tat-Tar 相互作用已被用作开发有效抗病毒药物的策略.因此,Hiv-1 Tar Rna 代表了治疗干预的范例系统.在此,我们使用生物素标记的 Tar Rna 从反应性叠氮化物和炔构建块池中组装其自己的配体.为了确定配体的结合位点和选择性,使用对照核苷酸(tar Dna 和不带凸出的 Tar Rna)模板进一步进行了原位环加成.使用链霉亲和素珠从生物素标记的靶模板中分离出命中的三唑连接的噻唑拟肽产品. Tar Rna 产生的主要三唑先导物可能结合在凸起区域,显示出对 Tar Rna 而非 Tar Dna 的特异性,并抑制 Tat-Tar 相互作用. DOI:10.1002/anie.202003461
专利号:WO-2024076331-A1 优先权日:2022-10-05 标题:HYDRAZINECARBOTHIOAMIDE AND 1,2,4-TRIAZOLE-3-THION DERIVATIVE COMPOUNDS CARRYING IMIDAZO[2,1-b]THIAZOLE RING AND SYNTHESIS METHODS OF THESE COMPOUNDS 发明人:GUZELDEMIRCI NURAY; DINCEL EFE DOGUKAN; YILMAZ OZDEN TUGBA; HASBAL CELIKOK GOZDE 权利人:ISTANBUL UNIV REKTORLUGU 摘要:In the invention, hydrazinecarbotioamide and 1,2,4-triazole-3-thion derivative compounds carrying an imidazo[2,1-b]thiazole ring, which have an inhibition activity on the alpha glucosidase (α-glucosidase) enzyme, and the synthesis methods of these compounds are described. The general structure of the molecules of the invention is shown by Formula (X).
专利号:WO-2011114184-A1 优先权日:2010-03-15 标题 :Amides of heterocyclic compounds as trpa1 inhibitors 发明人:CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 权利人:GLENMARK PHARMACEUTICALS SA; CHAUDHARI SACHIN SUNDARLAL; KUMAR SUKEERTHI; THOMAS ABRAHAM; PATIL NISHA PARAG; KADAM ASHOK BHAUSAHEB; WAGHMARE NAYAN TATERAO; KHAIRATKAR-JOSHI NEELIMA; MUKHOPADHYAY INDRANIL 摘要:Amides of heterocyclic compounds as Transient Receptor Potential subfamily A (TRPA) modulators are provided In particular, compounds described herein are useful for treating or preventing diseases, conditions and/ or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1) Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. (I).
专利号:US-4500716-A 优先权日:1981-11-19 标题 :Intermediate products for the preparation of Z-cephalosporins 发明人:KINAST GUENTHER 权利人:BAYER AG 摘要:Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: ##STR1## in which R 1 , R 4 and R 5 ae various organic radicals, n R 2 is alkoxycarbonyl, n Y is Cl, Br or --O--SO 2 --R 5 , and n X is a conventional cephalosporin substituent. n Many of the intermediates are new, especially in pure Z-form.
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
专利号:SU-1720490-A3 优先权日:1989-04-20 标 题 :Method of acylureidothiazol derivatives synthesis
专利号:TR-201615979-A2 优先权日:2016-11-08 标题:Synthesis and Antioxidant Activity of New Hydrazone Bearing Heterocyclic Ring Containing 4- [Bis- (2-Chlorethyl) Amine] Benzadehide