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1.
5-Silyl-substituted-2-furaldehyde thiosemicarbazones were prepared by the condensation of the corresponding furfurals or furfural diethylace-tals with thiosemicarbazide. The neurotropic activity of the synthesized thiosemicarbazones has been studied. The majority of the compounds examined possess high or medium neurotropic activity of the depressant type. They also show antihypoxic activity and decrease the duration of phenamine stereotype behaviour. Structure-activity correlation has been found. 相似文献
2.
Hiroyuki Miyamura 《Tetrahedron》2005,61(51):12177-12185
Highly active immobilized ruthenium catalysts, which can be used for oxidation of alcohols and sulfides, were developed on the basis of the polymer-micelle incarcerated (PMI) method. The catalysts could be recovered and reused several times without loss of activity and no metal leaching was observed. Selection of micelle-forming conditions and polymer structures were key in achieving high activities. TEM and SEM analyses were conducted to observe the structures of PMI-Ru. 相似文献
3.
The utility of acetylenic aldehydes in Baylis-Hillman reactions giving allyl propargyl alcohols in moderate to good yields is reported. 相似文献
4.
B.V. Subba Reddy B. Brahma Reddy K.V. Raghavendra Rao J.S. Yadav 《Tetrahedron letters》2010,51(43):5697-5700
1,3-Diaryl propargyl alcohols undergo smooth intramolecular Friedel-Crafts cyclization with triethylsilane in the presence of 10 mol % iodine 3-aryl-1H-indene derivatives in good yields in short reaction times. This is the first example on the synthesis of substituted indenes from 1,3-diaryl propargyl alcohols. The use of inexpensive and readily available molecular iodine makes this method quite simple, more convenient, and practical. 相似文献
5.
Lui Niimi Shuichi Hiraoka Tsutomu Yokozawa 《Journal of polymer science. Part A, Polymer chemistry》2005,43(22):5440-5448
Polyethers with propargyl side chains were synthesized by the acid‐catalyzed reaction of dialdehydes 1 , alkylene bis(trimethylsilyl) ethers 2 , and allenyltrimethylsilane 4 . When ethylene glycol bis(trimethylsilyl) ether was used as 2 , only oligomer was obtained. However, the use of 2 with longer carbon chains gave the desired polyethers consisting of 1 , 2 , and 4 in the molar ratio 1:1:2 in good yields in the presence of 10 mol % triphenylmethyl perchlorate (TrClO4) at ?20 °C. This polyether was treated with organometallic reagents such as Co complex or CuCl to give a cross‐linked polymer. This polymer synthesis is unusual in that it concurrently constructs both the polymer backbone and the functional side chains from three starting compounds. © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 43: 5440–5448, 2005 相似文献
6.
I. Iovel L. Golomba L. Zvejniece I. Shestakova E. Lukevics 《Chemistry of Heterocyclic Compounds》2003,39(4):449-454
We have synthesized the corresponding aldimines by condensation of 5-tert-butylfurfural and its trimethyl- and triethylsilyl analogs with 2-, 3-, and 4-trifluoromethylanilines in the presence of 4 molecular sieves. We have studied their neurotropic and antitumor activity. The phenamine motor activity test showed that tert-butyl derivatives exhibit high efficacy and also shorten the ethanol narcosis time. Some silyl derivatives exhibit significant anti-corazole activity. The tert-butyl derivatives have high cytotoxicity toward human lung fibrosarcoma cells (the 3-trifluoromethyl-substituted derivative) and mouse hepatoma cells (the 2-trifluoromethyl-substituted derivative). 相似文献
7.
This paper reports results obtained in a study on the palladium-catalyzed hydrostannation of substituted propargyl alcohols with the bulky trineophyltin hydride (1). The reaction of 1 with 10 propargyl alcohols containing one up to three substituents, was carried out in THF at room temperature leading to the corresponding allylstannanes following in all cases a syn addition stereochemistry. These additions took place in good to excellent yields and, mostly, with a high degree of stereoselectivity. The results obtained suggest that the observed α/β regioselectivity might be ascribed to the steric bulk of the proximal substituents rather than to electronic effects. Full 1H-, 13C-, and 119Sn NMR characteristics are included. 相似文献
8.
A method for one-pot preparation of Julia-Kocienski sulfides and sulfones from alcohols and thiols is reported. A variety of primary alcohols were converted to the corresponding mesylates by methansulfonyl chloride and triethylamine in THF. After the reaction is complete, thiol (1 or 10) and either NaH or t-BuOK were added. The Julia-Kocienski sulfides 3, 9 and 11 were prepared by one-pot two steps procedure from alcohols in 76–96% yields (16 examples). Furthermore, after the sulfide formation, the reaction mixture was neutralized by p-toluenesulfonic acid and treated with H2O2 and ammonium molybdate in EtOH to give the Julia-Kocienski sulfones 4 in good yields except for trans-2-hexen-1-ol. 相似文献
9.
10.
Enaminones are used as the key intermediates to construct heterocyclic compounds with various bioactivities. In this study, a simple and efficient approach for the synthesis of enaminones via amination of propargyl alcohols was developed. Under the catalysis of Ag2CO3, the reaction proceeded smoothly to afford the desired products in good yields. Preliminary mechanism experiments showed that Ag2CO3 played an essential role in the procedure of the reaction. 相似文献
11.
J. Bonet L. Callau J. A. Reina M. Gali V. Cdiz 《Journal of polymer science. Part A, Polymer chemistry》2002,40(22):3883-3892
We modified poly(epichlorohydrin) (PECH) with biphenyl carboxylic and naphthalene carboxylic acid derivatives which contains propargyloxy moieties. The linear polymers were characterized by NMR and IR spectroscopy, elemental analysis, DSC and TGA. We obtained only one side chain liquid crystalline. A smectic A mesophase of this biphenyl derivative was identified by DSC, light polarized optical microscopy and X‐ray diffraction. Thermal crosslinking of the aryl propargyl ether group via sigmatropic rearrangement took place while the material was in the isotropic phase. Partially curing this reactive liquid crystalline polymer resulted in the formation of an anisotropic elastomer when the curing was radically initiated in the range of mesophase stability. © 2002 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 40: 3883–3892, 2002 相似文献
12.
J.S. Yadav B.V. Subba Reddy N. Thrimurtulu N. Mallikarjuna Reddy A.R. Prasad 《Tetrahedron letters》2008,49(12):2031-2033
Aryl propargyl alcohols undergo smooth alkynylation with alkynylsilanes in the presence of 10 mol % of iodine under mild and neutral conditions to produce 1,4-diynes in excellent yields with high selectivity. The use of readily available molecular iodine makes this method simple, convenient, cost-effective and practical. 相似文献
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14.
A comprehensive overview on methods applied for syntheses of β-amino-α-trifluoromethyl alcohols, including stereocontrolled variants, is presented. In addition, reported cases of the exploration of β-amino-α-trifluoromethyl alcohols for the preparation of trifluoromethylated peptidomimetics and other biologically active, fluorinated compounds are discussed. Attractive opportunities for their applications as organocatalysts are also presented. 相似文献
15.
Sipyagin A. M. Enshov V. S. Kashtanov S. A. Potemkin V. A. Thrasher J. S. Waterfeld A. 《Russian Chemical Bulletin》2004,53(2):420-434
Thermolysis of xenon(ii) bis(perfluoroalkanecarboxylates) in the presence of diaryl disulfides occurs through the S—S bond cleavage to form dihalo-, halonitro-, and halodinitrophenyl perfluoroalkyl sulfides. The latter type of compounds was obtained for the first time. The main side process is the perfluoroalkylation of the aromatic ring. 相似文献
16.
Stefanie Berger 《Tetrahedron letters》2010,51(50):6630-6634
Monomeric ruthenium(0) complexes containing redox-coupled dienone ligands were found to catalyze the regio-selective addition of carboxylic acids or cyclic 1,3-dicarbonyl compounds to propargyl alcohols. 相似文献
17.
Mitsunori Honda Sho Sasaki Tsuyoshi Nishimoto Hiromoto Koshiro Ko-Ki Kunimoto Masahito Segi 《Tetrahedron letters》2018,59(42):3777-3781
The synthesis of cyclopropyl silyl ketones possessing a hydrocarbon group at 1-position of three-membered ring was investigated. The reaction of sulfoxonium ylide with α,β-unsaturated acylsilanes derived from α,β-unsaturated aldehydes did not afford the desired acylsilane derivatives. Instead, the corresponding silyl enol ethers were yielded exclusively. On the other hand, the Corey-Chaykovsky cyclopropanation of α-substituted α,β-unsaturated aldehydes proceeded well to give 1-substituted cyclopropyl aldehydes. The silyl substitution of formyl proton in the obtained aldehydes via umpolung of carbonyl group afforded the target acylsilanes. 相似文献
18.
Hydrozirconation of propargyl selenides afford(E)-3-selanyl vinylzirconocenes chlorides 2.Intermediates 2 reacted with aldehydes to obtain δ-selanyl allylic alcohols. 相似文献
19.
Alexander D. Dilman Dmitry E. Arkhipov Valentine P. Ananikov Vladimir A. Tartakovsky 《Journal of organometallic chemistry》2005,690(16):3680-3689
A general method for the synthesis of carbon-centered tris(pentafluorophenyl)silyl derivatives (RSi(C6F5)3) by reaction of trichlorosilanes (RSiCl3) with pentafluorophenylmagnesium bromide was described. The crystal structures of obtained compounds were studied by X-ray diffraction analysis (7 structures). The peculiarities of crystal packing were analyzed by means of DFT calculations. 相似文献
20.
Antonella Capperucci Alessandro Degl'Innocenti Tiziano Nocentini Giulio Castagnoli Irene Malesci Arianna Cerreti 《Phosphorus, sulfur, and silicon and the related elements》2013,188(5-6):1247-1251
Abstract Bis(trimethylsilyl)sulfide (HMDST) was demostrated to be a very efficient reagent in the delivery of sulfur functionalities, allowing us to synthesize a wide range of thiocarbonyl compounds. The most reactive derivatives were trapped with suitable dienes, leading to the synthesis of different heterocyclic molecules with an high degree of chemo- and regioselectivity. Recently, the mildness of this methodology also allowed us to obtain particularly reactive thiooxocompounds, such as thioformylsilanes, α,β-unsaturated thioaldehydes, thioketones, thioacylsilanes, and thioacylstannanes. 相似文献