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Synthesis of (Z)-4-hydroxytamoxifen and (Z)-2-[4-[1-(p-hydroxyphenyl)-2-phenyl]-1butenyl]phenoxyacetic acid 总被引:1,自引:0,他引:1
The synthesis of (Z)-4-hydroxytamoxifen and (Z)-2-[4-[1-(p-hydroxyphenyl)-2-phenyl]-1-butenyl]phenoxyacetic acid was accomplished using a McMurry reaction as the key step. The perfluorotolyl derivatives of the McMurry products enabled the separation of the minor undesirable geometrical isomer. The methodology proceeds without E,Z isomerization, employs a very mild final debenzylation step compatible with a large array of functional groups, and can be applied to the generation of a variety of 4-hydroxytamoxifen analogues. 相似文献
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A.R. Bailey R.E. Banks M.G. Barlow M. Nickkho-Amiry 《Journal of fluorine chemistry》1980,15(4):289-298
Caesium fluoride combined with perfluoro-1-azacyclohexene in acetonitrile to yield perfluoro-1-azacyclohex-1-ylcaesium (1), which was characterised by 19F n.m.r. spectroscopy and by treatment with iodomethane to give 2,2,3,3,4,4,5,5,6,6-decafluoro-1-methyl-1-azacyclohexane (2). Attempts to derivatize the caesium salt with chlorotrimethylsilane provided fluorotrimethylsilane, perfluoro-[1-(1-azacyclohex-1-en-2-yl)-1-azacyclohexane] (4), and 2-chloro-3,3,4,4,5,5,6,6-octafluoro-1-azacyclohexene (5); information on the course of this reaction was obtained through experiments in which perfluoro-1-azacyclohexene was shown to undergo conversion into its chloro-analogue (5) and its dimer (4) treatment with chlorotrimethylsilane and fluoride ion, respectively. Aluminium chloride also converts perfluoro-1-azacyclohexene into its chloro-analogue (5). 相似文献
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A. V. Tverdokhlebov Yu. M. Volovenko T. V. Shokol 《Chemistry of Heterocyclic Compounds》1998,34(1):44-50
A study has been made of the interaction of 2-[2-(benz)azolyl]3-keto-4-chlorobutanenitriles with primary aliphatic amines. This is a convenient method for the synthesis of 2-amino-3-[2-(benz)azolyl]-4(5H)-ketopyrroles.Tarasa Shevchenko Kiev University, Kiev 252601, Ukraine; e-mail dov@fosfor.kiev.ua. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 1, pp. 50–57, January, 1998. 相似文献
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Virgil Percec James H. Wang Shigeru Okita 《Journal of polymer science. Part A, Polymer chemistry》1992,30(3):429-438
The synthesis and the mechanism of oxidative polymerization of 2,2-bis[4-(1-naphthoxy)phenyl]propane ( 4 ) and 2,2-bis[4-(1-naphthyl)phenyl]propane ( 9 ) are presented. Both monomers polymerize by two different propagation steps. The first one represents a cation-radical dimerization of the naphthyl groups to dinaphthyl structure. H+[FeCl4]? generated from the first propagation step initiates a transalkylation reaction which provides structural units containing isopropylidenic groups inserted between phenyl and naphthyl, and between two naphthyl groups, respectively. Since the phenyl groups resulted from the second propagation reaction are unreactive in both the oxidative coupling and the transalkylation steps this polymerization reaction leads to polymers with low molecular weights containing phenyl chain ends. 相似文献
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A series of novel 1-glycosyl-4-{N-[(2'-morpholinethoxy)phenyl]aminomethyl}-1H-1,2,3-triazoles was designed and synthesized through a simple and efficient multistep synthetic method in good yields. The 1,2,3-triazole moiety acted as a single disubstituted ring and a linker between carbohydrates(D-glucose, D-galactose, maltose and lactose) and morpholine. The compounds were characterized by 1H NMR, 13C NMR and mass spectra(MS). Two different deprotection methods were discussed. The effects of compounds 5a, 5c and 6e on the intracellular calcium ion concentration([Ca2+]i) in the central neurons of S. exigua were well investigated by calcium imaging technique. The results demonstrated that compound 6e could elevate the calcium concentration in the glial cells, not in the neurons. 相似文献
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Eduardo Corts Roberto Martínez Martha B. Gutirrez Gmez 《Journal of heterocyclic chemistry》1991,28(5):1413-1415
The preparation of several 4-oxothiazolin-2-yl-indol-3-yl hydrazones is described. The structure of all products was corroborated by ir, 1H-nmr and mass spectrometry. 相似文献
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Grace A. Bennett Patricia A. Swift George B. Mullen Stanley D. Allen Jeffrey T. Mitchell Wendy E. Jones Vassil St. Georgiev 《Journal of heterocyclic chemistry》1989,26(6):1729-1734
The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)methyl]-3-[(1H-1,2,4-triazol-1-yl)-methyl]-2-methylisoxazolidines are described. The in vitro activity was evaluated in solid agar cultures against a variety of dermatophytes and yeast fungi, while in vivo activity was measured in an immune-compromised mouse model of systemic candidiasis. The activity of the title series was compared to that of ketoconazole and one derivative, the cis-3-(4-chlorophenyl)-5-(4-chlorophenyloxy)methyl analogue 5f was found to possess a similar potency in the in vivo assay. Structure-activity relationship correlations are also discussed. 相似文献
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George B. Mullen Patricia A. Swift David M. Marinyak Stanley D. Allen Jeffrey T. Mitchell C. Richard Kinsolving Vassil St. Georgiev 《Helvetica chimica acta》1988,71(4):718-732
The synthesis and antifungal activity of a novel series of 3-aryl-5-[(aryloxy)alkyl]-3-[(1H-imidazol-1-yl)-methyl]-2-methylisoxazolidines and related compounds, are discussed. The synthesis of the title compounds was accomplished via a 1,3-dipolar cycloaddition of α-substituted ketonitrones with l-alkenyl phenyl ethers (Scheme 2 and 3). The compounds were evaluated for in vitro antifungal activity in solid agar cultures against a broad variety of yeast and systemic mycoses and dermatophytes. While antifungal activity was evident throughout the series, in general, derivatives having halogen atom(s) in either or both aryl rings demonstrated the highest potency, especially against Trichophyton rubrum and Candida albicans. The dichloro analog 20 (PR 967-248) was found to possess the most useful activity. Its minimum inhibitory concentration (MIC) values ranged between 0.2 and 2.0 μg/ml, as compared to 0.2–20.0 μg/ml for the standard drug ketoconazole (4). 相似文献
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Reaction of the amines (CF3)2NX (X=Cl,Br) with norbornadiene either in solvent (CH2Cl2) at ?78 °C in the dark or in the vapour phase at 20 °C in daylight gives a mixture of 3-halogeno-5-(-bistrifluoromethylamino)nortricyclene (, -and , -isomers) and -5-(-bistrifluoromethylamino)- -7-halogenonorbornene in quantitative yield formed halonium ion addition to the diene. The reaction of the amine (CF3)2NBr in solvent Me2O or Et2O at ?78 °C in the dark gives the same products in low yield, together with 3-bromo-5-alkoxynortricyclene (, - and , -isomers) and the amine (CF3)2NR (R=Me, Et) in high yield. 相似文献
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A series of 5-phenylpyrrolo[2,1-c][1,4]benzoxazepines with basic substituents at the 11-position has been synthesized utilizing a nucleophilic aromatic fluoride displacement-cyclization. Piperidinyl derivatives were prepared by Vilsmeier formylation of the key 1-[(2-fluorophenyl)phenylmethyl]pyrrole ( 4 ) followed by addition of a piperidinyl Grignard reagent and cyclization of the resulting carbinol. A (dimethylamino)methyl derivative was prepared via an analogous cyclization of α-(dimethylamino)methyl-1-[(2-fluorophenyl)phenyl-methyl]-1H-pyrrole-2-methanol ( 10 ), obtained by the Hoeben-Hoesch acylation of 4 with chloroacetonitrile, addition of dimethylamine to the resulting α-chloroketone 8 , and reduction of the α-(dimethylamino)ketone 9 with sodium borohydride to give 10 . 相似文献
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Adam C. Alty Ronald E. Banks A. Ronald Thompson Haralambos S. Vellis 《Journal of fluorine chemistry》1988,40(2-3)
Coupling reactions of the type ArFN+2 + ArH → ArFN=NAr + H+ have been accomplished between fluorinated arenediazonium ions selected from the benzenic, pyridinic and pyrimidinic classes [ArF = C6F5, 4---CF3C6F4, 4---C5F4N, 4z.sbnd;C5F3N.Cl---3, 4---C5F2N.Cl2---3,5, 2---C5F3N.CF(CF3)2---4, 4---C4F3N2] and one or more aromatic compounds activated towards electrophilic attack (ArH = 1,3,5,---ME3C6H3, 1,3,5---Et3C6H3, MeOC6H6, and napth-2-ol). The diazonium ions were generated by addition of solid sodium nitrite to solutions of the amines ArFNH2 in anhydrous hydrogen fluoride, 80% hydrofluoric acid, or 98% sulphuric acid mixed with glacial acetic acid and propionic acid. This work has established that perfluorinated arenediazonium ions rank amongst the most electrophilic species of their general class. 相似文献
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2-Amino-4-[3-methyl-3-(5,6,7,8-tetrahydro-2-naphthyl)cyclobutyl]thiazole was synthesized by reaction of 1-methyl-1-(5,6,7,8-tetrahydro-2-naphthyl)-3-chloroacetylcyclobutane with thiourea in ethanol, and its subsequent transformations afforded new derivatives which were tested in vitro for antibacterial activity against some bacteria using the disk diffusion technique.__________From Zhurnal Organicheskoi Khimii, Vol. 40, No. 12, 2004, pp. 1861–1865.Original English Text Copyright © 2004 by Koparr, Cansz, Ahmedzade.The original article was submitted in English. 相似文献