CAS: 53406-38-5; 1-Aminoindole

该化合物是一种有机化合物,其特点是由诱导苯和火花环组成的单极结构,该化合物的特点是附附着于环第一个碳的氨基组(-NH2),使它成为丁醇的重要衍生物;在室内温度下,它一般是无色的,在黄色的黄色固体中无色,在水和酒精等极溶剂中可溶解;氨基组的存在使分子具有基本特性,使其得以参与各种化学反应,包括核生殖器替代和混合反应;1H-Indol-1-Amina因其潜在的生物活动,包括抗微生物和抗癌特性,对医药化学具有兴趣;此外,它作为合成更复杂的有机分子和药物的建筑块块,其反应性和结构特征使它在研究和工业应用中成为有价值的复合物.

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CAS号120-72-9 吲哚 | CAS号2950-43-8 羟胺-O-磺酸 | CAS号5470-18-8 2-氯-3-硝基吡啶 | CAS号133054-77-0 N-propylindol-1... | CAS号119257-33-9 N-(吡啶-4-基)-1H-吲哚-1-胺 | CAS号119257-34-0 Besipirdine | CAS号113698-47-8 N-indol-1-yl-1-...

合成工艺路线路线简述

  • 合成目标产物 1H-Indol-1-Amine 主要起始原料 2-Chloro-3-Nitropyridine
  • (文献来源)合成步骤主要原料 2-Chloro-3-Nitropyridine
📜吲哚置于hydroxylamine-O-Sulfonic Acid体系中,化学反应生成 1H-吲哚-1-胺
参考文献:1-[(咪唑啉丁-2-基)亚氨基]-1H-吲哚作为新的降压药:合成以及体内和体外生物学研究.
标题:1-[(咪唑啉丁-2-基)亚氨基]-1H-吲哚作为新的降压药:合成以及体内和体外生物学研究.
摘要:合成了一系列降压性α2-Ar激动剂的1-[(咪唑啉丁-2-基)亚氨基]-1H-吲哚类似物1-[(咪唑啉丁-2-基)亚氨基]-1H-吲唑,并在体外进行了测试因为它们在α1-和α2-肾上腺素受体以及咪唑啉i1和i2受体上的活性.最活跃的1-[((咪唑啉-2-基)亚氨基]亚氨基]-1H-吲哚显示对α1-和α2-肾上腺素受体具有高或中等亲和力,对咪唑啉-I1结合位点的α2-肾上腺素受体具有显着的选择性.吲哚衍生物3的体内心血管特性表明,在吲哚环的c-7位取代可能导致具有高心血管活性的化合物.其中,7氟同类物3G在该实验中显示出最明显的降压和心动过缓活性,剂量低至10杯/千克iv 使用体外和计算机方法确定所选的3型化合物的代谢稳定性.结果表明,这些化合物不易受到快速的第一阶段氧化代谢的影响.
DOI:10.1111/cbdd.12846

海关参考信息

专利信息


专利号:WO-2015193910-A1
优先权日:2014-06-20
标题:Asymmetric synthesis of 2-substituted indolines and 3-substituted cinnolines
发明人:KUMAR BOOPATHY SENTHIL; SUDALAI ARUMUGAM
权利人:COUNCIL SCIENT IND RES
摘要:The present invention relates to a novel one step proline catalyzed process for synthesis of chiral hydrazine and its derivatives from o-bromo hydro cinamaldehyde. Further, it relates to a novel one step process for the synthesis of substitued indolines and cinnolines from chiral hydrazines and its derivatives.

专利号:US-8026375-B2
优先权日:2007-04-13
标题:Transition metal catalyzed synthesis of N-aminoindoles
发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; RKYEK OMAR; URMANN MATTHIAS; ALONSO JORGE
权利人:SANOFI AVENTIS
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

专利号:US-2023212204-A1
优先权日:2020-01-16
标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds
发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI
权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST
摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.

专利号:US-11696954-B2
优先权日:2017-04-28
标题 :Synthesis of spherical nucleic acids using lipophilic moieties
发明人:KANG RICHARD; NALLAGATLA SUBBARAO; ANDERSON BART; KANDIMALLA EKAMBAR
权利人:EXICURE OPERATING COMPANY
摘要:Spherical nucleic acids (SNA) carrying self-aggregating oligonucleotides are described herein. Compositions of the SNA include discrete nanostructures that are not aggregated. Related methods are also described.

专利号:WO-2016075082-A1
优先权日:2014-11-10
标题:Stereoselective reductive amination of alpha-chiral aldehydes using omega-transaminases for the synthesis of precursors of pregabalin and brivaracetam
发明人:ZEPECK FERDINAND; NERDINGER SVEN; KROUTIL WOLFGANG; FUCHS CHRISTINE; SIMON ROBERT
权利人:SANDOZ AG
摘要:The present invention relates to processes comprising a combined racemization and stereoselective reductive amination step in which an aldehyde compound of formula (I) is contacted with an (R)-selective ω-transaminase or an (S)-selective ω-transaminase to racemize the compound of formula (I) and obtain an amine compound of formula (II). These processes are useful for the preparation of precursors of pharmaceutically active agents such as brivaracetam and pregabalin.

专利号:US-6512125-B1
优先权日:1994-05-13
标 题 :Preparation of 1H-indol-1-amines
发明人:LEE THOMAS B; GOEHRING KEITH E
权利人:AVENTIS PHARMA INC
摘要:The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.

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📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

合成参考文献


摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 336.
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 187.
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