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1,3,3-三甲基-2-亚甲基吲哚啉合成新工艺研究 总被引:2,自引:0,他引:2
1,3,3┐三甲基┐2┐亚甲基吲哚啉合成新工艺研究马新起李明静乔聪震(河南大学化学化工学院开封475001)侯希峰(开封化学试剂总厂475001)马新起男,33岁,讲师,从事化学工程教学精细化学品的开发与研究。河南省教委资助研究项目1997-06-3... 相似文献
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5 甲基吲哚是一种重要的化学中间体,在合成医药、染料等方面具有重要的作用[1]。传统合成方法路线较长、收率低、催化剂价格贵[2-5]。本文以对甲苯胺和环氧乙烷为原料,在铜系催化剂上一步合成5 甲基吲哚。反应方程式为:1 实验1 1 催化剂制备将硅胶放入箱式电炉中,以100℃/h的速度程序升温至900℃,恒温12h,自然冷却至室温进行扩孔。将扩孔硅胶置入0 2mol·L-1的Cu(NO3)2、0 05mol·L-1KNO3混合溶液中,浸渍24h取出,以120~130℃氮气流干燥,置入箱式电炉,500℃下煅烧2h取出,在氮气保护下冷却。将制得的催化剂装入Φ25mm的单管固定床… 相似文献
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报道了一种以N-甲基苯肼和3-甲基-2-丁酮为原料一步合成1,3,3-三甲基-2-亚甲基吲哚啉的新工艺。讨论了影响产品收率的各种因素。该新工艺具有原料易得,工艺路线较短,减少环境污染等特点。 相似文献
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Pt/TiO_2 was prepared by impregnation method and characterized with XRD、 BET and XRD results showed TiO_2 as prepared was anatase and the average particle sizewas about17 nm.The results of the photocatalytic degradation of 3- methyl indole suggested that the influences of Pt amount and loading amount of catalytics have obvious effect to catalyst activity.The concentration of flow rate and consistence obviously influenced the 3- methyl indole photocatalytic degradation. 相似文献
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在HF/6-31G(d)水平下, 对吲哚(A)与亚烷基丙二酸二甲脂(B)的Michael加成反应的机理进行了从头算理论研究. 计算结果表明, 该反应的机理为: A+B→分子复合物→TS1→IM→TS2→产物. 其中第一阶段由复合物经过渡态TS1生成中间体IM, 是C—C键的形成阶段, 该阶段的活化能垒较后一阶段要大, 是该反应的决速步骤; 第二阶段由IM经过渡态TS2生成产物, 完成H迁移和C—H键的形成. 反应过程中, 底物分子中离域化的π键电子的相互作用, 促进了 C—C新键的形成, 同时吲哚的共轭体系遭到部分破坏, 而体系经H迁移使新的C—H键形成后, 吲哚环的共轭体系又得到了恢复. 在MP2/6-311+G(d,p)水平下, 分别考虑乙醇和1,2-二氯乙烷的溶剂化效应, 单点能计算结果显示, 质子化溶剂对反应的影响较大, 不仅降低了反应的能垒, 且溶剂质子有可能参与了H迁移和C—H键的形成过程, 这一结论与实验结果一致. 相似文献
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利用二氯代磷酰基异氰酸酯与4,6-二甲氧基-2-氨基嘧啶的加成反应合成了中间体N-(4,6-二甲氧基嘧啶-2-基)-N'-二氯代磷酰基脲(Ⅰ).Ⅰ与2倍的醇或胺反应得到对称双取代磷酰基脲类化合物Ⅱa_Ⅱi;Ⅰ与1倍的胺反应得到氯代磷酰基脲类化合物Ⅲa_Ⅲe,再与1倍的醇反应则得到不对称双取代磷酰基脲类化合物Ⅳa_Ⅳg.生物活性测定结果表明,化合物Ⅱ、Ⅲ和Ⅳ均显示一定除草活性. 相似文献
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Prof. Chao Zheng, Prof. Shu‐Li You, Ping Yang and Dr. Ren‐Qi Xu (from left to right) 相似文献
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Javid Hussain Hidayatullah Khan Liaqat Ali Abdul Latif Khan Najeeb Ur Rehman Sajid Jahangir Ahmed Al‐Harrasi 《Helvetica chimica acta》2015,98(5):719-723
The phytochemical investigations on Cleome droserifolia resulted in the isolation and characterization of a new indole alkaloid, 5‐hydroxy‐2‐methoxy‐1‐methyl‐1H‐indole‐3‐carbaldehyde ( 1 ). The structure elucidation was carried out on the basis of 1D‐ and 2D‐NMR techniques. In addition to 1 , two known aromatic derivatives, veratrol ( 2 ) and 2‐methoxy‐4‐methylacetophenone ( 3 ), were also obtained. All these compounds were purified by repeated column chromatography of the CH2Cl2 fraction obtained from MeOH extract of Cleome droserifolia. The structure of the new compound 1 was finally confirmed by the combined 1D (1H‐ and 13C‐) and 2D (H? C correlations; HMBC and HSQC) NMR and IR spectroscopy, mass spectrometry (MS), and UV absorption spectroscopy techniques. The comparison of the physical and spectroscopic data with those in the literature provided evidence for the structure confirmation of known compounds. All the purified compounds were subjected to urease and α‐glucosidase enzymes inhibition. The results showed that compound 1 was more potent with an IC50 value 11.97±2.067 μg/ml towards urease inhibition, while the activity of α‐glucosidase enzyme was marginal. 相似文献
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乙酰基香豆素及其衍生物与吲哚的固相光反应研究 总被引:1,自引:1,他引:0
乙酰基香豆素及其衍生物与吲哚的固相光反应研究杜大明,王永梅,孟继本,周秀中张慧萍(南开大学化学系,天津,300071)(云南师范大学化学系)关键词香豆素,吲哚,固相光反应近年来固相光化学发展非常迅速,引起国内外学者的关注[1~3].我们研究了异种分子... 相似文献
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Hua Zhou Hong‐Ping He Ning‐Chuan Kong Yue‐Hu Wang Xiang‐Dong Liu Xiao‐Jiang Hao 《Helvetica chimica acta》2006,89(3):515-519
Three new indole alkaloids, 11,12‐de(methylenedioxy)danuphylline ( 1 ), methyl (2β,11β,12β,19α)‐6,7‐didehydro‐8,21‐dioxo‐11,21‐cycloaspidospermidine‐2‐carboxylate ( 2 ), and (2β,5β)‐aspidofractinin‐16‐ol ( 3 ) were isolated from Kopsia officinalis, together with 16 known compounds. Their structures were determined by spectroscopic methods. The isolated known compound (?)‐12‐methoxykopsinaline displayed antimanic effects in Drosophila, with an IC50 value of 12.5 μg/ml. 相似文献
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XueSenFAN XinYingZHANG YongMinZHANG GuiRongQU 《中国化学快报》2004,15(5):518-520
An efficient synthesis of 2, 3-disubstituted indole derivatives through low-valent titanium induced reductive cyclization of acylamido carbonyl compounds is described. 相似文献
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Yuan‐Zheng Cheng Qing‐Ru Zhao Xiao Zhang Shu‐Li You 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(50):18237-18242
Dearomatization of indoles provides efficient synthetic routes for substituted indolines. In most cases, indoles serve as nucleophiles. Reported here is an asymmetric dearomatization reaction of indole derivatives that function as electrophiles. The combination of a photocatalyst and chiral phosphoric acid open to air unlocks the umpolung reactivity of indoles, enabling their dearomatization with N‐hydroxycarbamates as nucleophiles. A variety of fused indolines bearing intriguing oxy‐amines were constructed in excellent yields with moderate to high enantioselectivities. Mechanistic studies show that the realization of two sequential single‐electron transfer oxidations of the indole derivatives is key, generating the configurationally biased carbocation species while providing the source of stereochemical induction. These results not only provide an efficient synthesis of enantioenriched indoline derivatives, but also offer a novel strategy for further designing asymmetric dearomatization reactions. 相似文献
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《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2017,129(1):122-127
The first enantioselective construction of a new class of axially chiral naphthyl‐indole skeletons has been established by organocatalytic asymmetric coupling reactions of 2‐naphthols with 2‐indolylmethanols (up to 99 % yield, 97:3 e.r.). This approach not only affords a new type of axially chiral heterobiaryl backbone, but also provides a new catalytic enantioselective strategy for constructing axially chiral biaryl scaffolds by making use of the C3‐electrophilicity of 2‐indolylmethanols. 相似文献
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Synthesis and Biological Activities of Some New Annulated Pyrazolopyranopyrimidines and Their Derivatives Containing Indole Nucleus 下载免费PDF全文
Anand R. Saundane Prabhaker Walmik Manjunatha Yarlakatti Vijaykumar Katkar Vaijinath A. Verma 《Journal of heterocyclic chemistry》2014,51(2):303-314
The key intermediate 6‐amino‐3‐methyl‐4‐aryl‐1‐(5′‐substituted‐3′‐phenyl‐1H‐indol‐2′‐carbonyl)‐1,4‐dihydropyrano[2,3‐c]pyrazol‐5‐carbonitriles 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i , 3j , 3k , 3l , 3m , 3n , 3o were prepared by cyclocondensation of 3‐methyl‐1‐(5′‐substituted‐3′‐phenyl‐1H‐indol‐2′‐carbonyl)‐5‐(4H)‐pyrazolones 1a , 1b , 1c with arylidine derivatives of malononitrile 2a , 2b , 2c , 2d , 2e . The compounds 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i , 3j , 3k , 3l , 3m , 3n , 3o were subjected to cyclocondensation reaction with formamide, formic acid, and carbon disulfide to afford the title compounds 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i , 4j , 4k , 4l , 4m , 4n , 4o , 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h , 5i , 5j , 5k , 5l , 5m , 5n , 5o , and 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j , 6k , 6l , 6m , 6n , 6o , respectively. The structures of all these previously unknown compounds were confirmed by their spectral studies and elemental analysis. These compounds were screened for their antimicrobial and antioxidant activities. 相似文献