CAS: 4342-03-4; 5- (3,3-Dimethyl-1-Triazenyl) Imidazole-4-Carboxamide

该化合物是一种主要用于治疗各种癌症,包括黑瘤和霍格金淋巴瘤的化疗治疗的抗乳粉剂,被归类为烷基剂,这意味着它干扰癌症细胞的DNA复制过程,最终导致细胞死亡.Dacarbazine是白到白的晶状粉,在水中溶解,分子重量相对较低.它的化学配方是C6H10N4O2S,并且经常通过静脉注射进行.该药物已知具有一系列副作用,包括恶心,呕吐和乳房抑制,这需要在治疗期间进行仔细监测.Dacarbazine通常与其他止血药结合使用,以提高其功效和改善患者的治疗结果.与所有乳液药剂一样,其使用应该由保健专业人员指导,考虑到特定癌症类型和病人健康状况.

结构式图片

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CAS号4656-86-4 1,5-二氢-4H-咪唑并[4... | CAS号56973-26-3 5-羟基-1H-咪唑-4-甲酰胺

合成工艺路线路线简述

  • 合成目标产物 Dacarbazine 主要起始原料 5-Amino-4-Imidazolecarboxamide And Dimethylamine
  • (文献来源)合成步骤主要原料 5-Amino-4-Imidazolecarboxamide 和 Dimethylamine

海关参考信息

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-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-7173021-B2
优先权日:2004-09-02
标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers
发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA
权利人:TIANJIN NORTH PHARM SCI TECH C
摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
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主要参考文献


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合成参考文献


参考文献:10.1093/neuonc/nop070
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参考文献:10.1158/1078-0432.ccr-11-0556
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参考文献:10.1007/s11060-011-0657-7
摘要:Lashkari HP, Saso S, Moreno L, Athanasiou T, Zacharoulis S. Using different schedules of Temozolomide to treat low grade gliomas: systematic review of their efficacy and toxicity. J Neurooncol. 2011 Nov;105(2):135–47. doi: 10.1007/s11060-011-0657-7.
参考文献:10.1038/bjc.2011.257
摘要:Eisen T, Marais R, Affolter A, Lorigan P, Robert C, Corrie P, Ottensmeier C, Chevreau C, Chao D, Nathan PD, Jouary T, Harries M, Negrier S, Montegriffo E, Ahmad T, Gibbens I, James MG, Strauss UP, Prendergast S, Gore ME. Sorafenib and dacarbazine as first-line therapy for advanced melanoma: phase I and open-label phase II studies. British Journal of Cancer. 2011 Jul 12;105(3):353–9. doi: 10.1038/bjc.2011.257.
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