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1.
Synthesis of potent adenosine A2A and A3 receptor agonist from the modification of adenosine-5′-N-ethylcarboxamide (NECA) has been reported. Diastereoisomer possessing an (R)-3,4-dihydro-2H-pyranyl (DHP) moiety exhibited the highest affinity at the A2A and A3 receptors. The key steps involve the synthesis of (R)-3,4-dihydro-2H-pyran-2-carboxaldehyde (7), which was obtained through the enzyme-catalyzed kinetic resolution of (±)-2-acetoxymethyl-3,4-dihydro-2H-pyran (5).  相似文献   

2.
Mercury(II) complex, [Hg((3,4-MeO-Bza)2En)I2] (I), where (3,4-MeO-Bza)2En = N,N′-bis(3,4-dimethoxybenzaldehyde)ethylenediimine, has been synthesized from the reaction of HgI2 with (3,4-MeO-Bza)2En in methanol as solvent at 50°C. It was characterized by elemental analysis (CHN), 1H-NMR spectroscopy and confirmed by single-crystal X-ray diffraction analysis. The complex I crystallizes in the monoclinic system, with space group P21/c, having one symmetry-independent Hg2+ ion coordinated in a distorted tetrahedral geometry by two N atoms of the Schiff base ligand and by two I atoms. The Schiff base ligand (3,4-MeO-Bza)2En acts as a chelating ligand and coordinates via two N atoms to the mercury center. It adopts an (E, E) conformation.  相似文献   

3.
G.C. Butchard  P.W. Kent 《Tetrahedron》1979,35(20):2439-2443
Addition of CF3OF to 3,4-di-O-acetyl-l-rhamnal gave four products separable by fractional crystallisation and column chromatography. The two principal products were in the epirhamnose series, i.e. trifluoromethyl 3,4-di-O-acetyl-2,6-dideoxy-2-fluoro-α-l-glucoside and 3,4-di-O-acetyl-2,6-dideoxy-2-fluoro-α-l-glucosyl fluoride. The lesser products were in the rhamnose series viz. trifluoromethyl 3,4-di-O-acetyl-2,6-dideoxy-2-fluoro-β-1-mannoside and 3,4-di-O-acetyl-2,6-dideoxy-2-fluoro-β-l-mannosyl fluoride. The structures were confirmed by 1H and 19F NMR spectral measurements. Deacylation and acidic hydrolysis gave the free 2-deoxy-2-fluoro sugars of both series.  相似文献   

4.
3-Alkynylquinoxaline-2-carbonitriles have been synthesized from 3-chloroquinoxaline-2-carbonitrile via the Sonogashira reaction. Treatment of 3-alkynylquinoxaline-2-carbonitriles with an alkylamine or ammonia has been shown to produce stable enamines, e.g., (Z)-3-(2-aryl-2-aminovinyl)quinoxaline-2-carbonitriles. Their base-induced cyclization gave the previously unknown pyrido[3,4-b]quinoxalin-1(2H)-imines or pyrido[3,4-b]quinoxalin-1-amines. 3-Alkynylquinoxaline-2-carbonitriles were directly transformed into pyrido[3,4-b]quinoxalin-1(2H)-imines by heating with an alkylamine and K2CO3 in DMF. The ionization constants, and absorption and fluorescent properties of the resulted pyrido[3,4-b]quinoxalin-1(2H)-imines were measured.  相似文献   

5.
The hydrothermal reactions of MnCl2·4H2O, 3,4-pyridinedicarboxylic acid (3,4-pydaH2) and triethylamine in aqueous medium yield two 3D metal-organic hybrid materials, [Mn(3,4-pyda)] (1) and [Mn3(OH)2(3,4-pyda)2(H2O)2] (2), respectively. In both complexes, each 3,4-pyda acts as a pentadentate ligand to connect five Mn(II) atoms via the pyridyl group and the two μ2-carboxylate groups (one in syn,anti-mode and one in syn-syn mode for 1 and both in syn,anti-mode for 2). Complex 1 possesses an interesting 3D coordination polymeric structure incorporating 1 D helical Mn(μ2-carboxylate)2 chain units, in which each Mn(II) atom is coordinated in less common square pyramidal geometry to four carboxylato oxygen atoms and one pyridyl nitrogen atom. Each 3,4-pyda links three helical Mn(μ2-carboxylate)2 chains and each Mn(μ2-carboxylate)2 chain is linked by other eight helical Mn(μ2-carboxylate)2 chains via sharing 3,4-pyda bridges. Complex 2 is a 3D coordination network consisting of 1D Mn3(OH)2 chains and 3,4-pyda bridges. The repeating trimeric structural unit in the manganese(II) hydroxide chain consists of two edge-sharing symmetry-related manganese octahedra linked via μ3-OH to a vertex of Mn2 octahedron. Each 3,4-pyda links three Mn3(OH)2 chains and each Mn3(OH)2 chain is linked by other six Mn3(OH)2 chains via 3,4-pyda bridges, resulting in a 3D coordination solid. Magnetic measurements reveal that a weak antiferromagnetic interaction between the MnII ions occurs in complex 1 and a 3D magnetic ordering at about 7.0 K in complex 2.  相似文献   

6.
The synthesis of cis- and trans-6-(trifluoromethyl)-3,4-dihydro-2H-thiopyran-3,4-diols from 6-(trifluoromethyl)-2H-thiopyran via an OsO4-catalysed dihydroxylation and bromohydroxylation-alkaline hydrolysis sequence is described. Acetylation of the diols followed by S-oxidation affords the corresponding cis- and trans-3,4-diacetoxy-6-(trifluoromethyl)-3,4-dihydro-2H-thiopyran S-oxides which reacted with acetic anhydride and boron trifluoride diethyl ether complex by an additive Pummerer pathway giving tetraacetyl derivatives of trifluoromethyl-containing thiopyranoses.  相似文献   

7.
The titanium-mediated cyclopropanation reaction using Ti(OiPr)3Me/EtMgBr/BF3·OEt2 has been applied to various 2-cyanopyrrolidines for the synthesis of functionalized 2-(1-aminocyclopropyl)pyrrolidine-3,4-diol derivatives (dideoxyiminoalditols). Under the same experimental conditions the trans-5-azidomethyl-2-cyanopyrrolidine derivative was not cyclopropanated but reduced into the corresponding 5-amino-2-cyano derivative. After polyol deprotection 2-(1-aminocyclopropyl)pyrrolidine-3,4-diols were obtained and their inhibitory activity towards 13 glycosidases has been evaluated. (2S,3S,4R,5S)-2-(1-Aminocyclopropyl)-5-methylpyrrolidine-3,4-diol (38), which has the same absolute configuration as l-fucose, is a moderate (IC50=44 μM), but selective, inhibitor of α-l-fucosidase from human placenta.  相似文献   

8.
2-Alkoxy-3,4-dihydropyrans were proved to be a class of powerful modular substrates to construct polyheterocycles by reacting with NH2-containing dinucleophiles, such as anthranilamide, 2-aminobenzenethiol, 1-(2-aminophenyl)pyrrole, and 2-(o-aminophenyl)indole in the presence of LiBr·H2O. A three-component reaction of isatoic anhydride, 2-alkoxy-3,4-dihydropyran and amine was also developed as well.  相似文献   

9.
Sterically hindered C2 chiral (3R,4R)- and (3S,4S)-2,2,5,5-tetraphenyltetrahydrofuran-3,4-diols have been conveniently prepared in a very high yield via heterogeneous intramolecular selective 1,4-cyclocondensation of (2R,3R)- and (2S,3S)-1,1,4,4-tetraphenylbutanetetraol in concentrated hydrohalic acids, respectively. Preliminary examination of additives for the Barbas–List reaction showed that in certain cases, the hindered C2 chiral tetrahydrofuran-3,4-diols were better chiral auxiliaries than enantiopure (R)- and (S)-1,1′-bi-2-naphthols.  相似文献   

10.
Biginelli reactions were performed using either ZrCl4 or ZrOCl2·8H2O as catalysts under neat conditions. Shorter reaction time than most of the classical methods was required when ZrCl4 was used. In general, 3,4-dihydropyrimidin-2(1H)-ones and thioxo-3,4-dihydropyrimidin-2(1H)-ones were obtained under neat conditions in moderate to good yields and good purity without using harmful solvents in the work up.  相似文献   

11.
[RuCl2(p-cymene)]2 efficiently catalyzes the rearrangement of 2-aryl-2-(phenylthio)penta-3,4-dienyl 2,2,2-trichloroacetimidate to afford (Z)-2,2,2-trichloro-N-(4-aryl-1-(phenylthio)penta-2,4-dien-2-yl)acetamide. Ru carbene is assumed as the reactive intermediate in this rearrangement.  相似文献   

12.
The use of KBH4-MgCl2 to reduce carboxylic acids and their derivatives to the corresponding alcohols or the respective reduced products is described. Methyl (S)-3,4-O-isopropylidene-3,4-dihydroxy butanoate 2 used as a reference substrate was reduced with KBH4 and MgCl2 in 1:1 mol ratio to (S)-1,2-O-isopropylidene-1,2,4-butanetriol 1.  相似文献   

13.
Substituted 2H-1,4-benzoxazines were synthesized from substituted 2-amino phenols and 1,2-dibromoethane using K2CO3 in good to excellent yields. The cyclized products were further reacted with alkyl bromides to obtain the desired N-substituted 3,4-dihydro-2H-1,4-benzoxazines.  相似文献   

14.
The superelectrophilic activation of N-aryl amides of 3-arylpropynoic acids by Bronsted superacids (CF3SO3H, HSO3F) or strong Lewis acids AlX3 (X=Cl, Br) results in the formation of 4-aryl quinolin-2(1H)-ones in quantitative yields. The vinyl triflates or vinyl chlorides may be formed as additional reaction products. The investigated amides in reactions with benzene give 4,4-diaryl 3,4-dihydroquinolin-2-(1H)-ones under the superelectrophilic activation. 4-Aryl quinolin-2(1H)-ones in POCl3 are converted into 4-aryl 2-chloroquinolines. 4-Fluorophenyl-4-phenyl 3,4-dihydroquinolin-2-(1H)-one give N-formylation products in a yield of 79% under the Vilsmeier–Haack reaction conditions.  相似文献   

15.
The 1,3-dipolar cycloaddition of unstabilized azomethine ylides with 2- and 3-nitroindoles furnishes the expected hexahydropyrrolo[3,4-b]indole cycloadducts in good to excellent yields. The cycloadducts can be denitrated with Bu3SnH/AIBN, and cycloadduct 5 was oxidized with MnO2 to yield the known pyrrolo[3,4-b]indole 13.  相似文献   

16.
4-Methyl- and 4-benzyl-5-aminoisoquinolin-1-ones are close analogues of the water-soluble PARP-1 inhibitor 5-AIQ. Their synthesis was approached through Pd-catalysed cyclisations of N-(2-alkenyl)-2-iodo-3-nitrobenzamides. Reaction of N,N-diallyl-2-iodo-3-nitrobenzamide with Pd(PPh3)4 gave a mixture of 2-allyl-4-methyl-5-nitroisoquinolin-1-one and 2-allyl-4-methylene-5-nitro-3,4-dihydroisoquinolin-1-one. N-Benzhydryl-N-cinnamyl-2-iodo-3-nitrobenzamide similarly gave 2-benzhydryl-4-benzyl-5-nitroisoquinolin-1-one and 2-benzhydryl-4-benzylidene-5-nitro-3,4-dihydroisoquinolin-1-one. The isomeric products are not interconvertible. A deuterium-labelling study indicated that the isomers were formed by different pathways: a π-allyl-Pd route and the classical Heck route. The corresponding secondary amides N-allyl-2-iodo-3-nitrobenzamide and N-((substituted)-cinnamyl)-2-iodo-3-nitrobenzamide gave good yields of the required 4-methyl- and 4-((substituted)-benzyl)-5-nitroisoquinolin-1-ones, respectively, under optimised conditions (Pd(PPh3)4, Et3N, Bu4NCl, 150 °C, rapid heating). Hydrogenation of the nitro groups gave 4-methyl- and 4-benzyl-5-aminoisoquinolin-1-ones, which were potent inhibitors of PARP-1 activity.  相似文献   

17.
《中国化学快报》2021,32(12):4033-4037
A visible-light-induced chemoselective reactions of quinoxalin-2(1H)-ones with alkylboronic acids in the presence of air (O2) and N2 atmosphere was developed under transition-metal free conditions, providing 3-alkylquinoxalin-2(1H)-ones and 3,4-dihydroquinoxalin-2(1H)-ones, respectively. The overall strategy accommodates a broad scope of substituted quinoxalin-2(1H)-ones and alkylboronic acids with good to excellent product yields.  相似文献   

18.
4-Aryl-6-methyl-3,4-dihydropyrimidin-2(1H)-one (DHPM) scaffolds of Biginelli type were oxidized using Co(II)/S2O82− and the reaction afforded 6-unsubstituted pyrimidin-2(1H)-ones through an unprecedented dealkylation process. 4-Alkyl DHPMs under similar conditions afforded yet another unusual product, ethyl tetrahydropyrimidin-2,4(1H,3H)-dione-5-carboxylate.  相似文献   

19.
Alkylation of 5-nitro-2-pyridone by alkenyl halides in acetone in the presence of K2СО3 proceeds with generation of a mixture of N- and О-derivatives with N-isomer prevailing. 1-Allyl- and 1-methylallyl-5-nitro-2-pyridone react with halogens with the formation of 2-halomethyl-6-nitro-2,3-dihydrooxazolo[3,2-a]-pyridinium halides. 1-Prenyl-5-nitro-2-pyridone reacts with bromine with the formation of 3-bromine-2,2-dimethyl-7-nitro-3,4-dihydro-2Н-pyrido[2,1-b][1,3]oxazinium bromide, and with iodine giving 2,2-dimethyl-7-nitro-3,4-dihydro-2Н-pyrido[2,1-b][1,3]oxazinium triiodide.  相似文献   

20.
The hydrothermal reactions of LnCl3·6H2O (Ln=Eu, Tb), pyridine-3,4-dicarboxylic acid (3,4-pydaH2), 1,10-phenthroline (phen) and NaOH in aqueous medium yield two metal-organic hybrid materials, [Eu2(3,4-pyda)3(phen)(H2O)·H2O]n (1) and [Tb2(3,4-pyda)3(phen)(H2O)·H2O]n (2), respectively. Both compounds have similar topology structure containing one-dimensional nano-chain, which is further assembled into a three-dimensional supramolecular network via π-π stacking interactions and hydrogen bonds. To the best of our knowledge, they represent the first example of nano-chain coordination polymers constructed by 3,4-pydaH2 and chelate heterocylic ligand. Interestingly, the 3,4-pyda anion exhibits three kinds of coordination modes in these complexes. The coordination modes of 3,4-pyda in complexes 1 and 2 have not been observed in other coordination polymers containing 3,4-pyda ligands. Compounds 1 and 2 exhibit strong fluorescent emission bands in the solid state at room temperature. Their magnetic analyses show that they exhibit different magnetic interactions.  相似文献   

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