CAS: 35302-72-8; 2,2,2-Trichloro-1-(1H-Pyrrol-2-yl)Ethanone

相似化合物

72652-32-5 183268-72-6 72652-31-4

吡咯,三氯乙酰氯置于tea体系中,用 二氯甲烷 用作溶剂,化学反应 6.0H,以80%的收率获得2-(三氯乙酰)吡咯
参考文献:新型吡咯并[2,1] [1,4]苯二氮卓-糖基化吡咯和咪唑聚酰胺共轭物的设计,合成和体外细胞毒性研究.
标题:新型吡咯并[2,1] [1,4]苯二氮卓-糖基化吡咯和咪唑聚酰胺共轭物的设计,合成和体外细胞毒性研究.
摘要:描述了新型吡咯并[2,1] [1,4]苯二氮杂-水不溶性31-38和水溶性39-46糖基化吡咯和咪唑聚酰胺共轭物的设计,合成和生物学评价,涉及氯化汞介导的相应环化反应氨基二乙基硫缩醛.为了提高pbd-聚酰胺共轭物的水溶性并探究最佳体外抗肿瘤活性的结构要求,制备了具有不同数量的含吡咯和咪唑的聚酰胺并掺入葡萄糖部分的化合物.这些化合物由美国国家癌症研究所针对60个人类癌细胞进行了测试,证明了水溶性pbd-聚酰胺化合物比现有的天然和合成吡咯并[2,1-C]具有更高的细胞毒性. 1,4]苯并二氮杂..这些化合物的乙酰化对应物水解后,其细胞毒性活性急剧增加.表1和表2中总结的活性数据表明,Pbd-聚酰胺的溶解度以及杂环的类型在影响pbd-聚酰胺缀合物的细胞毒性活性中起重要作用.与pbd-聚酰胺(水不溶型)结合物相比,Pbd-糖基化聚酰胺(水溶性)结合物39-46对许多人类癌细胞系具有高度的细胞毒性.
Doi:10.1039/b306685A

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:US-10919904-B2
优先权日:2016-08-17
标 题 :Northern-southern route to synthesis of bacteriochlorins
发明人：LIU YIZHOU; LINDSEY JONATHAN S; ALLU SRINIVASA RAO; FUJITA HIKARU
权利人:UNIV NORTH CAROLINA STATE
摘要:Described herein are chlorins, bacteriochlorins, methods and intermediates for the synthesis of bacteriochlorins, and methods of using such bacteriochlorins for, among other things, diagnostic and therapeutic purposes such as luminescent compounds in flow cytometry, and as active agents in photodynamic therapy (PDT).

专利号:US-RE49500-E
优先权日:2004-05-14
标 题:Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto
发明人：MARTINEZ BOTELLA GABRIEL; HALE MICHAEL; MALTAIS FRANCOIS; STRAUB JUDITH; TANG QING
权利人:VERTEX PHARMA
摘要:The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

专利号:US-8981092-B2
优先权日:2008-09-19
标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity
发明人：MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO
权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

专利号:US-2019256521-A1
优先权日:2016-08-17
标题:Northern-southern route to synthesis of bacteriochlorins

专利号:US-6545162-B1
优先权日:1996-02-26
标 题:Method for the synthesis of pyrrole and imidazole carboxamides on a solid support