CAS: 77716-11-1; 4-((Tert-Butoxycarbonyl)Amino)-1-Methyl-1H-Pyrrole-2-Carboxylic Acid

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1-(4-Bromo-1-Methyl-1H-Pyrrol-2-yl)-2,2,2-Trichloroethan-1-One置于copper(L) Iodide Lithium Hydroxide,Potassium Phosphate,N,N'-二甲基乙二胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇 作为反应溶剂,化学反应 58.0H,反应生成 4-(Boc-氨基)-1-甲基吡咯-2-羧酸
参考文献:的合成ñ-Methylpyrrole和ñ甲基咪唑氨基酸适用于固相合成
标题:的合成ñ-Methylpyrrole和ñ甲基咪唑氨基酸适用于固相合成
摘要:引入了新的和高产率的合成路线,以合成n-保护的n-甲基吡咯和n-甲基咪唑氨基酸,以规避与既定方案相关的困难.每个合成过程中的关键步骤包括铜介导的交叉偶联反应,以直接在n-甲基吡咯衍生物中安装氨基甲酸酯保护的4-胺,以及有效的硝化反应,然后在胺的合成中对胺进行一锅还原/ Boc保护.n-Me-咪唑氨基酸.
DOI:10.1021/jo048686R

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

专利号:US-2024360105-A1
优先权日:2021-08-04
标 题 :Process for polyamide synthesis
发明人：ZHANG CHENGZHI
权利人:DESIGN THERAPEUTICS INC
摘要:The disclosure relates to synthetic methods for producing polyamides, for example pyrrole and imidazole containing polyamides of Formula (I) or (II), or a pharmaceutically acceptable salts thereof. These polyamides bind genes having expanded oligonucleotide repeat sequences, which thereby modulates transcription. The disclosure further provides methods of modulation of the transcription of such DNA, and the use of polyamides as therapeutic agents to treat diseases associated with such DNA.

专利号:WO-9730975-A2
优先权日:1996-02-26
标题:Method for the synthesis of poly-pyrrole and poly-imidazole carboxamides on a solid support

专利号:US-6090947-A
优先权日:1996-02-26
标题:Method for the synthesis of pyrrole and imidazole carboxamides on a solid support

专利号:CN-1561333-A
优先权日:2001-08-30
标题 :Aromatic and Heteroaromatic Acid Halides for the Synthesis of Polyamides