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1.
Condensation of active methylene compounds with variously functionalized carbon two unit Michael acceptors (–) afforded the corresponding adducts, respectively. Reaction of such Michael adducts with NBS to afford the vinyl (, , and ) and ethynyl () bromides will also be described. 相似文献
2.
Hiroshi Onoue Masayuki Narisada Shoichiro Uyeo Hiromu Matsumura Kyo Okada Toshisada Yano Wataru Nagata 《Tetrahedron letters》1979,20(40):3867-3870
Allylazetidinones , , prepared by coupling of allylcoppers with chloroazetidinones , , were converted into carbapenem esters , – using an Emmons-Horner reaction to introduce the 6-side chain and an intramolecular Wittig reaction to form the carbapenem ring system. 相似文献
3.
The synthesis of the 2,4,6-cycloheptatrienyl ketones – by two alternative routes is reported: Route 1): The adducts from the phenyl(trimethylsiloxy)-acetonitriles , known as “umpolung” reagents, and tropylium tetrafluoroborate are cleaved by triethylammonium fluoride to form the aromatic cycloheptatrienyl ketones –. Route 2): the phenyl, methyl, and cyclopropyl ketone (, , ) are prepared by treatment of the acid chloride with the corresponding organomanganese iodides RMnI (, , ). The Fe-catalyzed coupling reaction of the acid chloride with a Grignard reagent was also used for the preparation of ketone . 相似文献
4.
Simon J. Edge W.David Ollis Julia Stephanidou Stephanatou J.Eraser Stoddart David J. Williams Kwamena A. Woode 《Tetrahedron letters》1981,22(23):2229-2232
The tri-3-methyltrianthranilide derivatives ()–() have been synthesised. Dynamic 1H n.m.r. spectroscopy indicates that the ,′,″-trimethyl derivative () exists in solution as slowly ring inverting ( ? *) enantiomeric helical conformations. X-Ray crystallography shows that the ,′-dimethyl-″-benzyl derivative () undergoes spontaneous resolution when it crystallises as a 1:1 adduct from toluene. The host molecules adopt a helical conformation (Figure 1) within a lattice structure that contains chiral channels (Figure 2) occupied by guest solvent molecules. 相似文献
5.
The 3β-acetoxy-16β,17β-epoxymethyleneandrost-5-ene () transforms into the dihydrooxazine condensed to the sterane skeleton (,,,,,) in a ring-expansion reaction with alkyl and aryl nitriles in the presence of HBF4— diethyletherate The 3β-acetoxy-16α, 17α-epoxymethyleneandrost-5-ene () undergoes a Wagner-Meerwein rearrangement under similar conditions. 相似文献
6.
Roshantha A.S. Chandraratna Robert R. Birge William H. Okamura 《Tetrahedron letters》1984,25(10):1007-1010
The electronic absorption spectra of the four new 12---locked retinals (1a–1d) bearing 7-, 11- double bond geometries are described and compared with those of analogous 7-, 11--geometries (1e–1h) and parent retinals (2a-h). 相似文献
7.
The synthesis of 3-acetylcyclohexanones , , has been realized by conjugate addition of lithiated cyanohydrin ether to 2-cyclohexenones , , in THF-HMPA, even if 3-substituted. 3-benzoylcyclohexanones , , are obtained from and , , in THF with excellent yields. 相似文献
8.
Reactivity of pyridazines , , , towards ethoxycarbonylradical (generated by redox decomposition of oxyhydroperoxide of ethylpyruvate) was studied. Application of this type of homolytic substitution for synthesis of hitherto not accessible pyridazine carboxylic acid esters , , , , , , , is demonstrated. In addition improved synthesis of diethyl 4,5-pyridazinedicarboxylate () is proposed. 相似文献
9.
Mikio Hori Tadashi Kataoka Hiroshi Shimizu Akihiko Tomoto 《Tetrahedron letters》1981,22(37):3629-3632
1-Benzoyl-2-methy1-3,4-dihydro-2-thianaphthalene () underwent novel intermolecular 1,4-rearrangement in refluxing toluene to give an enol ether , while rearrangement of 2-phenyl derivative proceeded intramolecularly in refluxing xylene to afford a 1,4-rearranged enol ether . On the other hand, ylides were refluxed in alcohols to afford some ring-opened products . 相似文献
10.
Inactive chaparrin has been converted in seven steps and in 16% overall yield to castelanone which is known to inhibit significantly growth of the murine lymphocytic leukemia P-388 cell line. The methodology developed has been applied to the preparation of quassinoid analogs , and . 相似文献
11.
The title reactions performed with (S)-α-amino acids or their derivatives as chiral sources were found to regioselectively give enantiomeric pairs of optically active 4-acetyl-3, 4-dimethyl-2-cyclohexenone (R)(+)- and (S)(?)-), 16–25% e.e., and those of optically active 6-acetyl-3,6-dimethyl-2-cyclohexenone((R)(+)- and (S)(?)-, 54–59% e.e., from the open chain triketone(). 相似文献
12.
The α-anions of 2-substituted 1,3-dioxolan-4-ones derived from chiral mandelic and lactic acid (, ; ; , ) were alkylated with high stereoselectivity. The products formed were hydrolysed to α-hydroxy acids with 65–85% e.e. ((S)(+)-,,, (R)(–)-). 相似文献
13.
Takehiko Nishio Katsuhiro Katahira Akira Kato Choji Kashima Yoshimori Omote 《Tetrahedron letters》1979,20(43):4211-4212
Irradiation of N-aryl-2(1H)-pyrimidin-2-ones (-) in a mixed benzene-alcohol solution afforded the products initiated by Type I cleavage, 1-(3-alkoxycarbonylamino-2-propene)-N-arylimines (-, , and ) in 45–51% yields. 相似文献
14.
The synthesis of five different 5,6-dideoxyhex-5-enofuranosides (, , and ) proceeds in 30–60% overall yield in two steps from commercially available 1--methyl pyranosides by reductive β-elimination of the intermediate 6-bromo-6-deoxypyranosides. 相似文献
15.
A. Stanley Jones Michael J. McClean Hironichi Tanaka Richard T. Walker Jan Balzarini Erik De Clercq 《Tetrahedron》1985,41(24):5965-5972
Reaction of 2',3'-secouridine with acetone gave the 3',5'--isopropylidene derivative (1) which upon treatment with mesylchloride gave the 2'--mesyl compound (2). Replacement of the mesyl group of 2 with halide could be effected by reaction with a metal halide in DMF. The 3',5'--isopropylidene group was removed simultaneously to give a 2'-halogeno-2'-deoxy-2',3'-secouridine. 2',3'-Dichloro-2',3'-dideoxy-2',3'-secouridine upon treatment with base gave 6()-chloromethyl-2()-(uracil-1-yl)-1,4-dioxane in addition to O2,2'-anhydro-3'-chloro-3'-deoxy-2',3'-secouridine, as previously reported. 2',3'-Dichloro-2',3'-dideoxy-5'-0-trityl-2',3'-secouridine was converted to 2',3'-dichloro-2',3'-dideoxy-2',3'-secocytidine (16) a triazole derivative. Compound 16 was unstable and appeared to form O2,2'-anhydro-3'-chloro-3'-deoxy-2,3'-secocytidine upon standing at room temperature. 5-Vinyl- and 5-() (2-bromovinyl) uridine dialdehydes have been made, as well as a number of other 5-substituted 2',3'-secouridine derivatives. None of the compounds obtained showed significant activity against a number of virus strains or tumor cell lines, except for 5-()(2-bromovinyl) uridine dialdehyde, which was inhibitory to the growth of human lymphoblast (Raji, Namalva) cells at a concentration of 28 μ/ml. 相似文献
16.
The phenols , , and , produced with remarkable regioselectivity by the cyclization of compounds and , have been converted to the benzindene prostaglandin analogs , , and , respectively. Compounds and are potent prostacyclin mimics. 相似文献
17.
Ylures sans sel,evolution en phosphoranes et equilibre ylure ⇌ phosphorane : I Synthese et structure
Synthesis of new salt-free ylids , to , , , , and and phoiphoranes , , , , , to by addition of a trivalent phosphorus compound (phosphites and amino-phosphines ) to with dimethyl acetylencedicartboxylate in presence of a protic trapping reagent are described. The results are consistent with trapping of carbanionic species. In relation with the. cyclic of acyclic structure of the triivalent phosphorus compound and the protic trapping reagent ie : methanol, phenol, carboxylic acid, etc.., several pathways are involved. Clearly), three phenomena are shown : one can obtain an ylid via a phosphorane or conversely a phosphorane via an ylid or an equilibrium Phoiphorane ? ylid. Results are dealing with thermodynamic or kinetically controlled reactions. 相似文献
18.
The conformations and the rotational barriers of the 2-substituted 1,3-diphenylallylanions – (Tab. 2) have been determined. Increasing size of the substituents leads to more ,- and ,-conformers at the cost of the ,-species. This trend is connected with decreasing ΔG3-value sof the rotational barriers; the barriers are essentially not affected by ion pair effects, which is in contrast to the parent “allyl anion”. 相似文献
19.
Tetracyclic azetidinones, and – were synthesized. In the cases of and, the main component was isolated from the two-component product of the cycloaddition. The minor component was concentrated to give a mixture, from which a computer technique utilizing the known spectrum of the main component gave the proton resonance spectrum also of the minor component. Only one diastereomer could be isolated for the each of the analogues–. Reaction of the 1,3-oxazine with chloroacetyl chloride gave, besides the azetidinone , the 1,3-oxazine [2,3-]-1,3-oxazin-4-one derivative. Configurations and conformations were determined by IR, 1H and 13C NMR spectroscopy. 相似文献
20.
The formation of the -bicyclo [6.1.0] nona-2,4,6-trienes - is not due to the sequence → → , which would involve the symmetry-forbidden reaction → even at ?50°C. Rather, reaction of RX at C4–7 of , which is formed together with , leads (probably via - and - to -. 相似文献