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Reaction of hydrazine with 5-(2-aryl-2-oxo-ethan-1-yl)-5-R Meldrum's acids 3 gives 4,6-disubstituted 4,5-dihydropyridazin-3(2H)-ones 4 at room temperature. The method is simple and the yield is good. The production of the starting material 3 also is discussed. 相似文献
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A new one-pot convenient preparation of 3,4-dihydro-4-imino-2(1H)-quinazolinones (4) is described by the reaction of 2-aminobenzonitriles (1) with chlorosulfonyl isocyanate (2), while the reaction of 1 with chlorocarbonyl isocyanate (6) affords ureidobenzonitriles (7), which on thermal cyclization gives 4. 相似文献
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1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸单甲酯(简称单甲酯,结构见图1)是1,4.二氢吡啶类药物的一个重要中间体。消旋二氢吡啶类药物很难直接进行化学拆分,光学纯的二氢吡啶类药物多利用单甲酯的单一对映体合成得到。Delee等将蛋白质类手性固定相用于高效液相色谱拆分单甲酯对映体。本文将Chiralpak AD-H直链淀粉氨基甲酸酯类手性固定相用于高效液相色谱直接对单甲酯对映体进行拆分,方法简便、快捷,分离效果较好。 相似文献
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N-Ethoxycarbonyl-4-pyridone is reduced to N-ethoxycarbonyl-4-oxo-1, 2, 3, 4-tetrahydropyridine by sodium borohydride in t-butyl alcohol containing ethyl chloroformate. Saponification of the product leads to 4-Oxo-1, 2, 3, 4-tetrahydropyridine. 相似文献
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B. Srinivasa Reddy A. Naidu P. K. Dubey 《Phosphorus, sulfur, and silicon and the related elements》2013,188(5):598-605
Abstract Condensation of 2-mercapto-3H-quinazolin-4-one (1) with chloroacetic acid gave 4-oxo-3,4-dihydroquinazoline-2-yl-sulfanyl)-acetic acid (2) that with anthranilamide (3) gave 2-(4-oxo-3,4-dihydroquinazolin-2-ylsulfanylmethyl)-3H-quinazolin-4-one (4). Oxidation of 4 with sodium hypochlorite in alkaline medium gave the novel product, 2-(4-oxo-3,4- dihydroquinazolin-2-ylsulfinyl methyl)-3H -quinazolin-4-one) (5). The entire sequences of reactions in this work have been carried out using eco-friendly solvents and green conditions. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
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ac-oxo-ketenedithioacetalsandrelatedcompoundsareversatileSynhlonsinorghocsynthesis.'"Althoughtherehavebeennumerousreportsaboutmisfieldinrecentyears,l-6allofthestUdiescanberoughlydividedintotwoaspectsfoneistheapplicahonofac-oxo-ketenedithioacetalsinorganicsyntilesis,andtileoilleristilesindiesontilereachvityadjustCdbythedialkylthiogroupsinac-oxo-betenedi1illoacetals.WehavedevotCdoureffortstothelatter."82-(l,2-ethylenedithio)medlylene-3-oxo-5-aryl-4-pentenoacids3wereformedbycondonsahonofacylketC… 相似文献
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3-R-Boc-amino-4-(2,4,5-trifluorophenyl)butyric acid (9) was obtained from L-methionine in six steps with a total yield of 32%. The α-amino acid segment of L-methionine was transferred to chiral aziridine by amino protection, reduction, hydroxyl derivation, and cyclization. After ring opening of 2,4,5-trifluoro-phenyl magnesium bromide, the methylthiomethyl group was then hydrolyzed to β-amino alcohol and oxidized to the target β-amino acid. 相似文献
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Krinochkin A. P. Shabunina O. V. Savchuk M. I. Kudryashova E. A. Rybakova S. S. Ladin E. D. Kopchuk D. S. Zyryanov G. V. Chupakhin O. N. 《Russian Journal of Organic Chemistry》2022,58(6):917-919
Russian Journal of Organic Chemistry - An efficient synthetic approach to 3-(4-carboxyphenyl)pyridine-2,6-dicarboxylic acid has been developed on the basis of “1,2,4-triazine”... 相似文献
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Sreenu Pavurala 《合成通讯》2014,44(5):583-588
An efficient synthesis of 3-(2-(4,5-dihydro-3,5-diphenylpyrazol-1-yl)thiazol-4-yl)-2H-chromen-2-one derivatives by a simple, atom-economical, and multicomponent reaction of chalcones, thiosemicarbazide, and 3-(2-bromoacetyl) coumarins in the presence of aqueous sodium hydroxide in refluxing ethanol is reported. The structures of newly prepared compounds have been confirmed by their analytical and spectral (IR, 1HNMR, 13CNMR and mass) data.
[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.] 相似文献
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New stereoisomeric N-bridged heterocycles, 4-oxo-1, 3-diazabicyclo-[3.3.0]octanes(4) were synthesized from trans-4-hydroxy-L-proline(1). Thiohydantoins 3 as the key intermediates were prepared by nucleophilic addition of 1 to isothiocyanates, and subsequent cyclization. These thiohydantoins 3 were readily desulfurized to provide 4. 相似文献
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A new synthesis of (2S,3R)-[3',3',3'-2H3]-valine has been completed and (2S,3S)-4-fluorovaline has been synthesised for the first time. Both compounds have been prepared by routes involving stereoselective addition to the (S)-pyroglutamate derivative and are available for studies in several areas of bio-organic chemistry. 相似文献
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Stereoselective diazotization of (S)-2-amino-2-phenyl acetic acid (L-phenyl glycine) (4) with NaNO2 in 6% H2SO4 in a mixture of acetone and water gave optically pure (S)-2-hydroxy-2-phenyl acetic acid (L-mandelic acid) (5). Esterification, gave (S)-2-hydroxy-2-phenyl acetic acid esters (6). The latter was treated with chloroacetyl chloride in the presence of triethylamine (TEA) in dichloromethane (DCM) to yield (S)-2-chloroacetyloxy phenyl acetic acid ester (2). In another sequence, the reaction of 2-(chloromethyl)-3-arylquinazolin-4(3H)-one (9) treated with N-Boc piperazine, followed by deprotection of the Boc group, to obtain 3-aryl-2-((piperazin-1-yl)methyl) quinazolin-4(3H)-one (3). Reaction of 2 with 3 in the presence of K2CO3 and KI gave the title compound, 2-(2-(4-((3,4-dihydro-4-oxo-3-arylquinazolin-2-yl)methyl)piperazin-1-yl) acetoyloxy)-2-phenyl acetic acid esters (1). The structures of all the new compounds obtained in the present work are supported by spectral and analytical data. 相似文献
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E. V. Resnyanskaya A. V. Tverdokhlebov A. A. Tolmachev Yu. M. Volovenko 《Russian Journal of Organic Chemistry》2005,41(2):257-260
A method was developed for preparation of 5-amino-4-(4-aryl-2-thiazolyl)-2,3-dihydro-2-pyrrolones by alkylation of 4-aryl-2-thiazolylacetonitriles by N-substituted chloroacetamides in the presence of K2CO3. In 1-(1-naphthyl)-substituted pyrrolones atropoisomerism was observed.__________Translated from Zhurnal Organicheskoi Khimii, Vol. 41, No. 2, 2005, pp. 266–269.Original Russian Text Copyright © 2005 by Resnyanskaya, Tverdokhlebov, Tolmachev, Volovenko. 相似文献
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(E)-2-(1-(2-Hydroxy-4-methoxyphenyl)ethylideneamino)-3-(4-hydroxyphenyl)methyl propionate (C22H27O6N, Mr = 401.45) has been synthesized by a condensation reaction of paeonol with tyrosin methyl ester hydrochloride, and its structure was determined by IR, NMR, HR MS and X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P21/c, with a = 11.91291(15), b = 9.49947(12), c = 19.8727(3) , β = 106.1104(15)°, V = 2160.60(5)3, Z = 4, Dc = 1.234 g/cm3, μ = 0.739 mm-1, F(000) = 856, R = 0.0466 and wR = 0.1461 for 3859 observed reflections with (Ⅰ> 2σ(Ⅰ)). In the crystal structure, the title compound is constructed by a centrosymmetric dimmer unit composed of a pair of π-π stacking enantiomers, and such units are linked by intermolecular O(5)-H(5)…O(1) and intramolecular N(1)-H(1)…O(1) hydrogen bonds. 相似文献
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Veneta Dryanska 《合成通讯》2013,43(2):203-209
Some 3-(2-benzothiazolyl)coumarin imines and 3-(2-benzothiazolyl)coumarins are prepared from 2-benzothiazolylacetonitrile and 2-hydroxybenzaldehydes in ethanol in the presence of catalytic amount of NaOH. 相似文献