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采用两种不同的途径合成了4-(5-甲醛基-2-噻吩基)-7-(2-噻吩基)[2,1,3]苯并噻二唑。研究结果表明,DMF/POCl3体系较n—BuLi/DMF体系产率更高。改变两种合成途径的反应条件,或用单醛化产物进一步醛化,均未发现二醛取代产物的生成。 相似文献
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以5-氨基-1,3-苯二甲酸和对叔丁基苯甲酰肼为原料合成了一种新型电致磷光材料中间体5-溴-1,3-二[2-(4'-叔丁基苯基)-1,3,4-噁二唑基-5)]苯,探讨了反应条件对合成反应的影响,反应的总收率为20.0%,方法可行. 相似文献
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Cyclization Reactions of 1-[2-amino-1-cyano-2-thio-]ethenepyridinium Ylides 1-[2-Amino-1-cyano-2-thio-]ethene-pyridinium ylides 1 can be alkylated with methyliodide or α-haloesters and α-haloketones, respectively, to form 1-[2-alkyl(aryl)amino-1-cyano-2-methylthio-ethene-1]pyridinium iodides 2a-–e or 1-[2-alkyl(aryl)-amino-1-cyano-2-alkoxy(aryl)-carbonylmethylthio-ethene-1] pyridinium salts 3a–f . With the exception of 3a–b the compounds 3 or 1 react with haloketones to yield 1-[4-amino-2-alkyl-(aryl)amino-5-benzoyl-thiene-3]pyridinium salts 4a–m or 3-alkyl-4-aryl-2-(1-cyano-1-pyridinium)methylene-Δ4-thiazoline salts 5a–f . 相似文献
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Yingfang He Dr. David M. Whitehead Dr. Emmanuelle Briard Dr. Shin Numao Dr. Linjing Mu Prof. Roger Schibli Prof. Simon M. Ametamey Dr. Yves P. Auberson 《ChemMedChem》2020,15(24):2448-2461
We describe here our efforts to develop a PET tracer for imaging GluN2A-containing NMDA receptors, based on a 5H-thiazolo[3,2-α]pyrimidin-5-one scaffold. The metabolic stability and overall properties could be optimized satisfactorily, although binding affinities remained a limiting factor for in vivo imaging. We nevertheless identified 7-(((2-fluoroethyl)(3-fluorophenyl)amino)-methyl)-3-(2-(hydroxymethyl)cyclopropyl)-2-methyl-5H-thiazolo-[3,2-α]pyrimidin-5-one ([18F] 7b ) as a radioligand providing good-quality images in autoradiographic studies, as well as a tritiated derivative, 2-(7-(((2-fluoroethyl)(4-fluorophenyl)amino)methyl)-2-methyl-5-oxo-5H-thiazolo[3,2-α]pyrimidin-3-yl)cyclopropane-1-carbonitrile ([3H2] 15b ), which was used for the successful development of a radioligand binding assay. These are valuable new tools for the study of GluN2A-containing NMDA receptors, and for the optimization of allosteric modulators binding to the pharmacophore located at the dimer interface of the GluN1-GluN2A ligand-binding domain. 相似文献
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[Al]-, [Ga]- and [Fe]-HZSM-5 having closely similar Brønsted acid site densities were prepared. The low-temperature adsorption of H2 and D2 was studied by FTIR spectroscopy and the frequency shifts ΔνOH and ΔνHH (ΔνDD) were measured and compared with corresponding frequency shifts observed for CO and N2 probes. A linear correlation between |ΔνOH|1/2 which is proportional to the heat of formation &;/Delta;HB of the H-bonded complex O-H···B (B representing the H-bond acceptor), and the proton affinities of the three probe molecules was found for [Al]-HZSM-5. The ΔνOH-values measured for CO and H2 (D2) on the three isomorphously substituted zeolites suggested the following acid strength ranking: [Al]-HZSM-5 > [Ga]-HZSM-5 ≈ [Fe]-HZSM-5. This sequence is clearly reflected in the relative activities of the materials for the acid-catalyzed disproportionation of ethylbenzene. 相似文献
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A convenient and efficient regioselective synthesis of new pyrimido[4′,5′:4,5] [1,3]thiazino[3,2-a]perimidines is described through intermolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 1H-perimidine-2(3H)-thione in short reaction times under mild conditions. 相似文献
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《Journal of Sulfur Chemistry》2013,34(6):595-603
Reaction of 5-(4-chlorophenyl)-2-thioxo-2,3-dihydro-1H-indeno[2',1':5,6] pyrido[2,3-d]pyrimidine-4,6-dione with hydrazonoyl chlorides gave 1,2,4-triazolo[4,3-a]pyrimidine derivatives regioselectively in good yields. The structures of the newly synthesized compounds are established on the basis of chemical and spectroscopic evidence as well as their synthesis by alternative methods. 相似文献
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以 4′ 氯哌醋甲酯为原料,研究了作为潜在的治疗可卡因滥用症的药物———4 羟基- 5- (4′- 氯苯基 )双环 [4,4, 0]- 1 氮杂癸烷的合成。4′- 氯哌醋甲酯首先用乙酸酐在室温下进行乙酰基化,然后在 -70℃下经二异丙基胺锂(LDA)作用关环得中间产物(±)- threo -2, 4 -二氧代- 5- (4′- 氯苯基)双环[4, 4, 0] -1 氮杂癸烷,产率 60%。中间体先用硼氢化钠在甲醇中室温下选择性地将酮羰基还原,粗产物经V(石油醚)∶V(乙酸乙酯) =1∶1重结晶后,在四氢呋喃中于回流温度下用乙硼烷 四氢呋喃络合物进一步还原酰胺基,得到(±) threo 4α 羟基- 5 -(4′- 氯苯基 )双环[4, 4, 0]- 1 氮杂癸烷,两步产率为 67%。所得α位羟基产物经过Swern氧化,然后在四氢呋喃中在 -78℃下用三(仲丁基)硼氢化钾选择性还原,立体专一性地得到 (±) threo- 4β 羟基- 5 (4′- 氯苯基 )双环 [4, 4, 0]- 1 氮杂癸烷,氧化 还原反应总产率为 70%。 相似文献
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对(Z)-2-甲氧基-5-[2-(3,4,5-三甲氧基苯基)乙烯基]-苯胺(AVE-8063)的合成进行了研究。采用两条路线得到AVE-8063,均以对甲氧基苯乙酸为起始原料,经硝化、Perk in缩合、还原得到(E)-2-(3-氨基-4-甲氧基苯基)-3-(3,4,5-三甲氧基苯基)-丙烯酸(Ⅳ),直接脱羧得到目标化合物(路线1);为改善后处理操作条件,还将化合物Ⅳ的氨基保护、再经脱羧及去保护得到目标化合物(路线2)。路线1和路线2的总收率分别为20.4%和17.1%,均高于文献报道的W ittig反应路线,各中间体及产物结构经MS、IR以及1HNMR确证。 相似文献