CAS: 155815-95-5; 4-Amino-1H-Pyrrole-2-Carboxylic Acid

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4-硝基吡咯-2-羧酸 4-Nitropyrrole-2-Carboxylic Acid 5930-93-8

📜4-硝基吡咯-2-羧酸置于palladium-Carbon 乙醇体系中,用 乙醇,水 用作溶剂,化学反应 2.0H,以to Give The Title Compound (0.35 G,88%)的收率获得4-氨基吡咯-2-羧酸
参考文献:Antibiotic Carbapenem Compounds
标题:Antibiotic Carbapenem Compounds
摘要:本发明涉及碳青霉烯,并提供式(i)的化合物:##str1## 其中:R1是1-羟基乙基,1-氟乙基或羟甲基;R2是氢或c1-4烷基;R3是氢或c1-4烷基;A是一个5元杂环芳基环,其中包含一个氮原子和最多两个其他杂原子,选自氮,氧和硫;并通过环中的碳原子与连接的氨基甲酰基团的氮原子相结合,通过环中的碳原子上的羧基取代,并在环中的碳原子上可选择进一步取代;在任何环中--Nh--中,H可选择被c1-4烷基替换;或其药学上可接受的盐或体内水解酯.还描述了它们的制备过程,制备中间体,作为治疗剂的使用以及含有它们的制药组合物.

专利信息

专利号:US-7449547-B2
优先权日:2003-06-03
标题:Process for the synthesis of distamycin and derivatives thereof using 1-methyl-4-formylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate
发明人：LOMBARDI PAOLO
权利人:NAXOPHARMA S R L
摘要:A process for the total synthesis of Distamycin, and synthetic poly-(4 aminopyrrole-2-carboxamide) congeners thereof, using 1-methyl-4-forinylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate, is provided. The process finds application for both in solution and solid support synthetic technologies.

专利号:US-7067622-B2
优先权日:2001-06-25
标题 :Method of the solid phase synthesis of pyrrole-imidazole polyamide
发明人：SUGIYAMA HIROSHI; IIDA HIROKAZU; SAITO ISAO; SAITO TAKASHI
权利人:JAPAN SCIENCE & TECH AGENCY
摘要:It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.

专利号:WO-0196313-A1
优先权日:2000-06-14
标 题:Distamycin a analogs
发明人：BOGER DALE L
权利人:SCRIPPS RESEARCH INST; BOGER DALE L
摘要:The development of a solution-phase synthesis of distamycin A and its extension to the preparation of 2640 analogs are described. Thus, solution-phase synthesis techniques with reaction workup and purification employing acid/base liquid-liquid extractions were used in the multistep preparation of distamycin A (8 steps, 40 % overall yield) and a prototypical library of 2640 analogs providing intermediates and final products that are ≥ 95 % pure on conventional reaction scales. Screening the prototypical library provided compounds that are 1000 times more potent than distamycin A in cytotoxic assays (67, IC50 = 29 nM, L1210), that bind to poly[dA]-poly[dT] with comparable affinity, and that exhibit an altered DNA binding sequence selectivity. Several candidates were identified which bound the five base-pair AT-rich site of the PSA-ARE-3 sequence, and one (128, K = 3.2 x 106 M-1) maintained the high affinity binding (K = 4.5 x 106 M-1) to the ARE-consensus sequence containing a GC base-pair interrupted five base-pair AT-rich site suitable for inhibition of gene transcription initiated by hormone insensitive androgen receptor dimerization and DNA binding characteristic of therapeutic resistant prostate cancer.

专利号:US-2009264300-A1
优先权日:2005-12-01
标题 :Enzymatic encoding methods for efficient synthesis of large libraries

专利号:US-2007060523-A1
优先权日:2003-06-03
标 题:Process for the synthesis of distamycin and derivatives thereof using 1-methyl-4-formylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate

专利号:EP-1641753-B1
优先权日:2003-06-03
标题:Process for the synthesis of distamycin and derivatives thereof using 1-methyl-4-formylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate