共查询到20条相似文献,搜索用时 109 毫秒
1.
以三聚氯氰作为反应促进剂,在室温和CH3CN作为溶剂的条件下,利用取代2-氨基吡啶、醛和烷基异腈三组分缩合,高收率地实现了一系列咪唑并[1,2-a]吡啶类化合物的合成.产物结构经1H NMR,13C NMR和元素分析等进行了表征. 相似文献
2.
3.
4.
5.
6.
7.
8.
以1-氯乙酰基愈创兰烃奠和取代2-氨基吡啶为原料,一锅法合成了一系列未见文献报道的1-{2-咪唑[1,2-a]吡啶基}愈创兰烃薁衍生物,收率47% ~ 74%,其结构经1H NMR,IR和元素分析表征. 相似文献
9.
无溶剂条件下,用氨基磺酸催化芳香醛,2-氨基苯并咪唑和β-二羰基化合物的三组分反应,简单而方便地得到了苯并[4,5]咪唑并[1,2-a]嘧啶类衍生物.该法具有产率高,成本低廉,环境友好,适应性广简捷方便等优点. 相似文献
10.
11.
A series of novel 5,7-diphenylimidazo[1,2-a]pyridine derivatives was designed and synthesized. The in vitro cytotoxic activities of all the target compounds against human colorectal cancer(HT-29), human lung can- cer(H460), human gastric cancer(MKN45) and human breast cancer(MDA-MB-231) cell lines were evaluated. The pharmacological results indicated that most of the target compounds showed moderate to excellent activities against the tested cell lines. The most promising compound 4h(0.20, 0.006, 0.08, 0.021 μmol/L) was 2.6, 5.1, 3.6 and 21.9 times more active than EPC2407(0.52, 0.031, 0.29, 0.46 μmol/L) against HT-29, H460, MKN45 and MDA-MB-231 cell lines, respectively. 相似文献
12.
Kiyoshi Tanaka Takashi Takeyama Ryousuke Yukawa Satoru Iwata Tohru Kurushima 《Supramolecular chemistry》2013,25(3):186-193
ortho-Azacrown-substituted (tetrafluorophenyl)imidazo[1,2-a]pyridine (2) in an acetonitrile solution emits 380 nm light in the presence of Li+ cation and emits 460 nm light in the presence of Zn2+, Mg2+ or H+ cation. In contrast, para-azacrown-substituted analogue (1) emits three different fluorescent lights responding to Li+, Zn2+ or H+ cation, respectively; 388 nm light to Li+ cation, 433 nm light to Zn2+ cation or 469 nm light to H+ cation. 相似文献
13.
N. O. Saldabol J. Popelis V. A. Slavinskaya 《Chemistry of Heterocyclic Compounds》2001,37(8):1021-1024
Vilsmeier formylation of 2-(2-furyl)-substituted imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine, and also 6-(2-furyl)imidazo[2,1-b]thiazole with 1 mole of reagent occurs at the free position of the imidazole ring, while with an excess of the reagent it also occurs at the position 5 of the furyl group. 相似文献
14.
15.
3-Ethoxycarbonyl-5-methyl-1-(4-methylphenyl)-4-pyrazoloylhydroximoyl chloride (1) reacted with o-phenylenediamine, o-aminothiophenol, o-aminophenol and methyl anthranilate to afford 3-nitrosoquinoxaline, benzothiadiazine, benzoxadiazine, and 3-hydroxyquinazoline, respectively. Imidazo[1,2-a]pyridine, imidazo[1,2-a]pyrimidine and isoxazole derivatives were obtained via the reaction of 1 with 2-aminopyridine, 2-aminopyrimidine and the appropriate active methylene compounds, respectively. Pyrazolo[3,4-d]pyridazines, and pyrrolidino[3,4-d]isoxazolines derivatives were also synthesized. The structures of the newly synthesized compounds were established on the basis of spectral data and alternate synthesis whenever possible. 相似文献
16.
Samvel N. Sirakanyan Domenico Spinelli Athina Geronikaki Victor Kartsev Elmira K. Hakobyan Anthi Petrou Ruzanna G. Paronikyan Ivetta M. Nazaryan Hasmik H. Akopyan Anush A. Hovakimyan 《Molecules (Basel, Switzerland)》2021,26(11)
Background: Neurotic disturbances, anxiety, neurosis-like disorders, and stress situations are widespread. Benzodiazepine tranquillizers have been found to be among the most effective antianxiety drugs. The pharmacological action of benzodiazepines is due to their interaction with the supra-molecular membrane GABA-a-benzodiazepine receptor complex, linked to the Cl-ionophore. Benzodiazepines enhance GABA-ergic transmission and this has led to a study of the role of GABA in anxiety. The search for anxiolytics and anticonvulsive agents has involved glutamate-ergic, 5HT-ergic substances and neuropeptides. However, each of these well-known anxiolytics, anticonvulsants and cognition enhancers (nootropics) has repeatedly been reported to have many adverse side effects, therefore there is an urgent need to search for new drugs able to restore damaged cognitive functions without causing significant adverse reactions. Objective: Considering the relevance of epilepsy diffusion in the world, we have addressed our attention to the discovery of new drugs in this field Thus our aim is the synthesis and study of new compounds with antiepileptic (anticonvulsant) and not only, activity. Methods: For the synthesis of compounds classical organic methods were used and developed. For the evaluation of biological activity some anticonvulsant and psychotropic methods were used. Results: As a result of multistep reactions 26 new, five-membered heterocyclic systems were obtained. PASS prediction of anticonvulsant activity was performed for the whole set of the designed molecules and probability to be active Pa values were ranging from 0.275 to 0.43. The studied compounds exhibit protection against pentylenetetrazole (PTZ) seizures, anti-thiosemicarbazides effect as well as some psychotropic effect. The biological assays evidenced that some of the studied compounds showed a high anticonvulsant activity by antagonism with pentylenetetrazole. The toxicity of compounds is low and they do not induce muscle relaxation in the studied doses. According to the study of psychotropic activity it was found that the selected compounds have an activating behavior and anxiolytic effects on the models of “open field” and “elevated plus maze” (EPM). The data obtained indicate the anxiolytic (anti-anxiety) activity of the derivatives of pyrimidines, especially pronounced in compounds 6n, 6b, and 7c. The studied compounds increase the latent time of first immobilization on the model of “forced swimming” (FST) and exhibit some antidepressant effect similarly to diazepam. Docking studies revealed that compound 6k bound tightly in the active site of GABAA receptor with a value of the scoring function that estimates free energy of binding (ΔG) at −7.95 kcal/mol, while compound 6n showed the best docking score and seems to be dual inhibitor of SERT transporter as well as 5-HT1A receptor. Conclusions: Тhe selected compounds have an anticonvulsant, activating behavior and anxiolytic effects, at the same time exhibit some antidepressant effect. 相似文献
17.
We unfold a rapid synthetic protocol for the preparation of imidazo[1,2-a]pyridine in cyclohexane. This methodology includes several advantages like shorter reaction time, catalyst free, broader substrate scope, and good yields of the desired products. Late stage functionalization of imidazo[1,2-a]pyridine has also been performed through C–H bond activation and C–C cross-coupling reactions. 相似文献
18.
Meenakshi Budhiraja Prof. Amjad Ali Dr. Vikas Tyagi 《European journal of organic chemistry》2023,26(11):e202201426
Herein, we describe an efficient strategy for the construction of enzyme-metal biohybrid catalyst [Pd(0)-CALB@SiO2] via encapsulation of Candida antarctica lipase B and Pd(0) within silica. Next, the applicability of the newly constructed biohybrid was demonstrated by catalyzing the sequence of Groebke-Blackburn-Bienayme (GBB) multicomponent reaction and Suzuki-Miyaura coupling in a single-pot to produce clinically significant imidazo[1,2-a]pyridine derivatives. Interestingly, both entities, i.e., CALB enzyme and Pd(0)-metal of hybrid catalyst, exhibited good catalytic activity during this approach. Further, the generality of this protocol was explored by using differently substituted boronic acid, which gave related products in 49–87 % isolated yield. Next, the synthetic utility was proved by set-up a gram scale reaction which provided the complementary product in 81 % yield. Also, the developed biohybrid was found to be reusable up to five catalytic cycles. 相似文献
19.
Synthesis of pyrimido[1,2-a]benzimidazole and pyrano[2,3-c]pyrazole derivatives were achieved using polyethylene glycol (PEG-400) as promoting reaction medium in water under catalyst-free conditions at reflux and room temperature, respectively. The structure of pyrimido[1,2-a]benzimidazole was confirmed using 1H NMR, 13C NMR, DEPT, and HMBC experiments. The promising points for the present methodology are efficiency, generality, high yield, short reaction time, cleaner reaction profile, ease of product isolation, simplicity, potential of recycling reaction medium, and finally agreement with green chemistry protocols. 相似文献
20.
A series of imidazo[1,2-a]pyrimidine derivatives substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized in order to improve their anti-inflammatory activities. Biological tests suggested that these compounds have antiinflammatory activities with COX-2 selectivity to some extent. 相似文献