CAS: 765-39-9; 1H-Pyrrol-1-Amine

相似化合物

937046-95-2 616-43-3 1551-06-0

上下游产品

CAS号885-12-1 2-(1H-吡咯-1-基)异吲... | CAS号109-97-7 吡咯 | CAS号7531-52-4 L-脯氨酰胺 | CAS号937046-95-2 (1H-吡咯-1-基)氨基甲酸叔丁酯 | CAS号647841-44-9 2-(pyrrol-1-yla... | CAS号38602-81-2 1-pyrrol-1-ylpyrrole

吡咯置于氢氧化钾,Hydroxylamine-O-Sulfonic Acid体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 1.0H,以38%的收率获得产物1-氨基吡咯
参考文献:取代的(吡咯并氨基)吡啶类:治疗阿尔茨海默氏病的潜在药物.
标题:取代的(吡咯并氨基)吡啶类:治疗阿尔茨海默氏病的潜在药物.
摘要:合成了一系列新的取代的(吡咯并氨基)吡啶,并在体外(抑制[3H]奎宁环烷基苯磺酸盐结合)和体内(逆转东pol碱引起的痴呆)评估了化合物的拟胆碱性质.治疗阿尔茨海默氏病.表现出显着活性的化合物得到了更广泛的评估,从而揭示了理想的肾上腺素活性成分的存在.介绍了该系列化合物的合成和构效关系,以及所选化合物的生物学特征.
DOI:10.1021/jm950644V

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-6541653-B2
优先权日:2001-04-26
标题 :Synthesis of carbamate through low pressure heterogeneous oxidative carbonylation of amines
发明人：CHUANG STEVEN S C; CHI YAWU; CHEN BEI; TOOCHINDA PISANU
摘要:The process disclosed herein satisfies the need in the art for an industrially viable oxidative carbonylation catalytic system, and is capable of producing carbamates at a significantly higher rate than those processes reported in journal and patent literature. This reaction process takes place via a reaction mechanism that does not involve drastic conditions. Specifically, the catalytic system of the present invention employs Group VIII metal catalysts and/or copper-based catalysts with halide promoters to produce carbamates through heterogeneous oxidative carbonylation at atmospheric pressure and relatively non-drastic temperatures in a gas-solid carbonylation process.

专利号:US-7087378-B1
优先权日:1996-02-26
标 题 :Design, synthesis and use of specific polyamide DNA-binding ligands
发明人：BAIRD ELDON E; DERVAN PETER B
权利人:CALIFORNIA INST OF TECHN
摘要:The invention encompasses improved selective polyamides for binding to specific nucleotide sequences of double stranded DNA as well as methods for designing and synthesizing polyamide DNA binding ligands that are selective for an identified specific nucleotide sequence. The 3-hydroxy-N-methylpyrrole/N-methylpyrrole carboxamide pair specifically recognizes the T•A base pair, while the N-methylpyrrole/3-hydroxy-N-methylpyrrole pair recognizes A•T nucleotide pairs. Similarly, an N-methylimidizole/N-methylpyrrole carboxamide pair specifically recognizes the G•C nucleotide pair, and the N-methylpyrrole/N-methylimidizole carboxamide pair recognizes the C•G nucleotide pair.

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-5684160-A
优先权日:1989-11-17
标 题:3-aminopyrroles, methods for their synthesis and for their pharmaceutical use
发明人：SCHARFENBERG PETER; LIEBSCHER JUERGEN; KNOLL ALEXANDER; USCHMAJEW ALEKSEJ; ROLFS ANDREAS; LOHMAN DIETER; FAUST GOTTFRIED; MORGENSTERN EVELINE
权利人:ARZNEIMETTELWERK DRESDEN GMBH
摘要:The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles. n Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents. n The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations. n Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

专利号:US-2002183541-A1
优先权日:2001-04-26
标题:Synthesis of carbamate through low pressure heterogeneous oxidative carbonylation of amines