共查询到20条相似文献,搜索用时 15 毫秒
1.
We report a facile one-pot, three-step synthesis of N-(4-(2-aminopyridin-4-yl)thiazol-2-yl)-2-phenylacetamides via condensation of 2-p-methoxybenzylamino-4-acetylpyridine with phenylacetylthioureas. 相似文献
2.
Nicolas Lebouvier Typhanie Corbin Guillaume Le Baut Marc Le Borgne 《Tetrahedron letters》2006,47(36):6479-6483
New conazole antifungals, in the series of triazole alcohols 23a-d and 24a-e incorporating an indole moiety substituted at 5-position by halogens, a cyano or 4-methoxyphenyl group, have been synthesized by ring opening of corresponding oxiranes 15 and 16. These dihalogeno intermediates and their congeneers could be prepared in high yields by Corey-Chaykovsky reaction under microwave irradiation. 相似文献
3.
Allyn T. Londregan Gregory Storer Ceshea Wooten Xiaojing Yang Joseph Warmus 《Tetrahedron letters》2009,50(17):1986-1988
Dehydrative amide couplings with 2-pyridylamines suffer from variable yields. A mild and high-yielding synthesis of N-(pyridin-2-yl)amides employing 2-aminopyridine-N-oxides is presented as a solution. 相似文献
4.
Adri van den Hoogenband Jack A.J. den Hartog Jos H.M. Lange Jan Willem Terpstra 《Tetrahedron letters》2004,45(46):8535-8537
A novel efficient synthetic route to the pharmaceutical key intermediate N-(piperidin-4-yl)-1,3-dihydroindol-2-one is described. The key step involves a high-yielding intramolecular palladium-catalyzed amination reaction using Buchwald’s X-Phos ligand under mild reaction conditions. 相似文献
5.
A very concise synthesis of a potent KDR kinase inhibitor 1 is described. The synthesis features an exceedingly efficient one-pot preparation of the aminothiazole 6 followed by Pd-Xantphos catalyzed cross-coupling with chloropyridine aldehyde 11. Reductive amination of the resulting aldehyde 10 with the piperazine fragment 9 afforded the final product. 相似文献
6.
Yuefen Zhou 《Tetrahedron letters》2004,45(43):8049-8051
A general method was developed to synthesize a class of N-(4-oxo-2-substituted-4H-quinazolin-3-yl)-substituted sulfonamides in moderate to good yield. This new method can be applied in both single compound and parallel synthesis. About 90 compounds with a variety of substituents were synthesized using this method in a parallel fashion. 相似文献
7.
Mouhamad Jida Mohamad Soueidan Nicolas Willand Francine Agbossou-Niedercorn Lydie Pelinski Guillaume Laconde Rebecca Deprez-Poulain Benoit Deprez 《Tetrahedron letters》2011,52(14):1705-1708
A facile and rapid synthetic approach of N-benzyl-2-substituted piperazine building-blocks via an Ugi strategy is described. This strategy is high yielding (80-92% overall yield), step-efficient and fast using microwave heating and tert-butylisocyanide as a convertible isocyanide. This method is useful for the obtention of key intermediates in medicinal chemistry. 相似文献
8.
The one-pot synthesis of a novel class of N-(4-hydroxyquinolin-2-yl)sulfonamide derivatives is achieved in moderate to good yields by the sequential copper-catalyzed reaction between sulfonyl azides, terminal alkynes, and isatoic anhydride in N,N-dimethylformamide. 相似文献
9.
The microwave assisted thionation of 3-substituted 4-imino-oxazolidin-2-ones with hydrogen sulfide in dichloromethane-pyridine afforded 3-substituted 4-thioxo-oxazolidin-2-ones. 相似文献
10.
Vadim V. Negrebetsky Peter G. Taylor Sergey Yu. Bylikin Alexander G. Shipov Yuri I. Baukov 《Journal of organometallic chemistry》2006,691(19):3976-3988
Eleven new silicon-substituted N-(dimethylsilylmethyl)- and N-(methylphenylsilylmethyl)amides and -lactams bearing a chiral carbon in the amide or lactam fragment, and containing the OSiC3X (X = Hal, OTf) coordination fragment have been synthesized and their structures determined in solution by spectroscopic means. These structures are consistent with the hypervalency model. Quantum chemical calculations adequately reflect correlations between the type of monodentate ligand X and the geometric parameters of the N-C-O-Si-X fragments.The activation parameters for enantiomerization and diastereomerization in these new compounds and the other related compounds were determined by the dynamic NMR (DNMR) method using full line-shape analysis. The free activation energy values in the absence of external nucleophiles vary from 9 to 27 kcal mol−1. The entropies of activation (ΔS#) are negative (−20 to −50 cal mol−1 K−1) in all cases except for the chloride derivatives of 4-phenyl-2-pyrrolidone and 4-oxazolidinone that have weaker intramolecular O → Si coordination. Irregular mechanisms of permutational isomerization were proposed on the basis of the DNMR data and the results of quantum-chemical calculations carried out by ab initio (HF) and DFT (PBE, B3PW91, 6-311++G(d,p)). Depending on the coordination environment at silicon, the mechanisms proposed involve either the dissociation of the Si-X bond followed by the Berry pseudorotation or similar in the intermediate or the cleavage of intramolecular O-Si bond with subsequent inversion at the silicon atom. The apparently simple pseudorotation mechanism involving only the pentacoordinate structures 1-21 does not appear to be favoured in any of the examples studied. 相似文献
11.
In the course of developing a method for the parallel synthesis of purin-9-yl-acetamides, it was found that microwave irradiation was beneficial in accelerating the nucleophilic displacement of halogens by amines at the C-2 position of the purine nucleus. 相似文献
12.
《Arabian Journal of Chemistry》2014,7(6):972-975
We want to achieve the synthesis of 3-(1H-benzoimidazol-2-yl)-7-(diethylamino) coumarin-2-one (1), 3-(1H-benzoimidazol-2-yl)-7-(dimethylamino) coumarin-2-one (2), 3-(1H-benzoimidazol-2-yl) coumarin-2-one (3) that are important dyes in industries (Soko owska et al., 2001). Methods for the synthesis of some of these compounds have been the title in some pervious patents, but enough information about separation and purification of them was not clearly indicated. We carried out several methods for the synthesis of the mentioned compound and purification with different yields. Now, we can synthesise these dyes under microwave irradiation in solid phase and solvent free methods with 80% yield, which is a high and remarkable percentage. 相似文献
13.
A practical procedure for the synthesis of 3-fluorooxindole derivatives having basic amine moieties was developed, which involves Selectfluor™-mediated oxidative fluorination of N,N-dialkyltryptamines in the presence of Lewis acid. This procedure was applied to an antimigraine drug, rizatriptan, to afford the corresponding 3-fluorooxindole, which is a potential fluorine-containing drug candidate. 相似文献
14.
Hanumant B. Borate Sangmeshwer P. Sawargave Suleman R. Maujan 《Tetrahedron letters》2009,50(47):6562-6566
A short synthetic strategy for 3,6-disubstituted-N-2-thienyl/aryl-indoles, involving reaction of substituted 2,4-difluoro/dichloro-styrene epoxide with substituted 2-formylaminothiophenes or substituted N-formylanilines in the presence of a base followed by treatment with an acid, has been developed. The method was applied for the synthesis of a number of indoles with a variety of substituents at 1, 3, and 6 positions of the indole moiety. 相似文献
15.
This paper describes the selective syntheses of two cis-isomer-enriched cyclopentanone fragrances: (Z)-3-(2-oxopropyl)-2-(pent-2-en-1-yl)cyclopentanone (four steps, 62% overall yield, 67% cis) and Magnolione® (five steps, 60% overall yield, 55% cis). In addition, the asymmetric synthesis of (3aR,7aS)-5-methyl-2,3,3a,4,7,7a-hexahydro-1H-inden-1-one as well as (3a′R,7a′S)-5′-methyl-2′,3′,3a′,4′,7′,7a′-hexahydrospiro[[1,3]dioxolane-2,1′-indene] has been realized by an efficient kinetic resolution, which enables the selective synthesis of the 2S,3R-isomer-enriched 3 and 4. 相似文献
16.
Substituted 2-(N-alkylamino)-pyrimidin-4-ones were synthesized from N-alkyl β-amino acid esters starting with guanidinylation using Pbf-activated thiourea. The six-membered pyrimidinones were obtained in good yields via intramolecular cyclization during TFA cleavage of the Pbf protecting group. 相似文献
17.
Sonogashira coupling of (E)-α-iodovinylstannanes 1 with (trimethylsilyl)acetylene gave (Z)-1-(trimethylsilyl)-3-(tributylstannyl)alk-3-en-1-ynes 2, which underwent a desilylation reaction to afford (Z)-3-(tributylstannyl)alk-3-en-1-ynes 3 in high yields. (1E,3Z)-1-Halo-3-(tributylstannyl)-substituted 1,3-dienes 5 could be synthesized stereoselectively via hydrozirconation of (Z)-3-(tributylstannyl)alk-3-en-1-ynes 3, followed by trapping with iodine or NBS. 相似文献
18.
19.
A new effective approach to the synthesis of some new (Z)-5-(substituted)-2-thioxothiazolidin-4-one 3a–l and (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one 5a–l is reported under microwave irradiation as well as conventional conditions. 相似文献
20.
Zhen Li Chengtao Fang Yannan Zheng Guanyinsheng Qiu Xiaofang Li Hongwei Zhou 《Tetrahedron letters》2018,59(44):3934-3937
A switchable synthesis route is developed for benzo[d]oxazole derivatives and (2-hydroxylaryl)benzamide from 2-hydroxylbenzeneketoxime using organomolecules (BOP-Cl, and CNC) and Lewis acid cocatalyzed Beckmann rearrangement (BR) reaction. Further, this reaction is switched using different organocatalysts. 相似文献