CAS: 4461-33-0; Benzoylisocyanate

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苯甲酰氯置于ammonium Hydroxide体系中,用 二氯甲烷,1,2-二氯乙烷 作为反应溶剂,化学反应 3.5H,反应生成 苯甲酰异氰酸脂
参考文献:含有酰肼-Hydr和羧酰胺基团的新型1,3-噻唑衍生物的合成,抗肿瘤活性和作用机理
标题:含有酰肼-Hydr和羧酰胺基团的新型1,3-噻唑衍生物的合成,抗肿瘤活性和作用机理
摘要:合成了一系列新颖的2,4,5-三取代1,3,3-噻唑衍生物,其中包括酰肼-肼,以及包括46个化合物t的羧酰胺部分,并评估了它们在体外对五种人类癌细胞系的抗肿瘤活性.18种标题化合物t对mcf-7,Hepg2,Bgc-823,Hela和a549细胞系的抑制活性高于5-Fu.尤其是,T1,T26和t38表现出最佳的ic 50细胞毒性活性分别针对mcf-7,Bcg-823和hepg2细胞系的2.21μg/ Ml,1.67μg/ Ml和1.11μg/ Ml值.这些结果表明,1,3-噻唑,酰肼-Hydr和羧酰胺部分的组合对细胞毒性活性非常有利.此外,流式细胞仪分析表明,化合物t1和t38可以诱导hepg2细胞凋亡,并证实t38通过s细胞周期停滞诱导了细胞凋亡的诱导.
DOI:10.1016/j.Bmcl.2016.05.059

专利信息

专利号:US-4756739-A
优先权日:1985-12-21
标题 :Pyridine derivatives and the N-oxides thereof, and the use thereof as intermediates for the synthesis of plant protecting agents
发明人：FUSS ANDREAS; KOCH VOLKER
权利人:HOECHST AG
摘要:The compounds of the formula I (I) in which A denotes N or N->O, Z denotes O or NH, R denotes H, (halo)alkyl, (halo)alkenyl, (halo)alkynyl or alkoxycarbonyl, R1 denotes hydrogen, halogen, amino, -NHOH, hydroxyl, (substituted) phenylazo or a radical of the formulae Y=C=N-, Y1Y2C=N-, Y3NH- or K denotes 0 or 1, and m and n, independently of one another, denote a number from 1 to 4, with the proviso that, when Z-R denotes OH or NH2, (R1)n denotes at least one radical of the formula or represents two radicals, in the 5 or 6 position of the heterocyclic ring, which, in the 5 position, denote halogen and, in the 6 position, denote a radical of the group comprising halogen, amino, hydroxyl or phenylazo, which may be substituted as specified above, are valuable intermediates in the synthesis of plant protection agents.

专利号:US-2009099218-A1
优先权日:2007-09-17
标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (bpu) sulfur analogs
发明人：KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO
权利人:KHAN SAEED R; HALLUR GURULINGAPPA; HIDALGO MANUEL; JIMENO ANTONIO
摘要:This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines.

专利号:US-6232462-B1
优先权日:1994-08-30
标题:Reduction of nonspecific hybridization by using novel base-pairing schemes
发明人：COLLINS MARK L; HORN THOMAS; SHERIDAN PATRICK J; WARNER BRIAN D; URDEA MICHAEL S
权利人:BAYER AG
摘要:Methods are provided for substantially reducing background signals encountered in nucleic acid hybridization assays. The method is premised on the elimination or significant reduction of the phenomenon of nonspecific hybridization, so as to provide a detectable signal which is produced only in the presence the target polynucleotide of interest. In addition, a novel method for the chemical synthesis of isoguanosine or 2′-deoxy-isoguanosine is provided. The invention also has applications in antisense and aptamer therapeutics and drug discovery.

专利号:US-7595326-B2
优先权日:2005-04-18
标题 :Synthesis of novel tubulin polymerization inhibitors: benzoylphenylurea (BPU) sulfur analogs
发明人：KHAN SAEED R; HALLUR GURULINSAPPA; HIDALGO MANUEL; JIMENO ANTONIO
权利人:CHAMPIONS BIOTECHNOLOGY INC
摘要:A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6 n and 7 d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6 n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6 n retained significant ability to inhibit tubulin assembly, with an IC 50 of 2.1 μM.

专利号:US-7153967-B2
优先权日:2002-07-23
标题:Preparation of 1H-imidazo [4,5-C] quinolin-4-amines via 1H-imidazo [4,5-C] quinolin-4-phthalimide intermediates
发明人：MERLI VALERIANO; MANTOVANI SILVIA; BIANCHI STEFANO
权利人:TEVA GYOGYSZERGYAR ZARTKOERUEE
摘要:The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.

专利号:US-7335772-B2
优先权日:2002-07-26
标 题:1H-imidazo [4,5-c] quinolin-4-cyano and 1H-imidazo [4,5-c] quinolin-4-carboxamide intermediates
发明人：MERLI VALERIANO; MANTOVANI SILVIA; BIANCHI STEFANO
权利人:TEVA GYOGYSZERGYAR ZARTKOERUEE
摘要:The invention relates to a process for the synthesis of 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1 H-imidazo[4,5-C]quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C]quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c]quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C]quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c]quinoline 4-carboxamide, and to the said intermediates.