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1.
As part of our investigations in the field of the α-halogenated imine chemistry,1 we describe herein a convenient and general synthesis of aliphatic α-halogenated imidoyl cyanides 1 (X=Cl,Br). From the synthetic and mechanistic point of view, compounds 1 are expected to exhibit interesting features due to the presence of three functional groups in the molecule. 相似文献
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S. K. Moiseev M. A. Cherevatskaya T. A. Verbitskaya I. V. Glukhov A. S. Peregudov V. N. Kalinin 《Russian Chemical Bulletin》2012,61(10):1933-1942
The synthesis of 1-[(2-R-o-carboran-1-yl)methyl]benzotriazoles (R = Me, Ph) is described. α-Deprotonation of these compounds followed by reactions of the generated carbanions with MeI give the corresponding α-methylated products. Even at room temperature, they exist in solution as an equilibrium mixture of two conformers due to steric crowding around the Cα atom. In contrast, the anions generated by deprotonation of α-ferrocenyl derivatives of 1-methyl- and 1-ethylbenzotriazoles are ambident and are attacked by electrophiles at both the Cα and N(3) atoms. 相似文献
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Total synthesis of Phytophthora mating hormone α1 (1) has been demonstrated. The required stereochemistries (methyl) are achieved by applying CuI-(S)-Tol-BINAP-catalyzed conjugate addition of Grignard reagents to α,β-unsaturated esters. 相似文献
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A. V. Varlamov A. N. Levov F. Toze A. I. Chernyshev 《Chemistry of Heterocyclic Compounds》2004,40(4):490-495
Condensation of 1-amino-4-azafluorene with -diketones and with unsaturated ketones in basic medium gives novel substituted 1,4-diazafluoranthenes and also dihydro-4-azafluoreno[9,9a,1-b,c]cyclohexano[2',3'-e]- and indano[1',2'-e]azepines. 相似文献
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《Tetrahedron: Asymmetry》2000,11(8):1681-1685
The title compounds, valuable chiral synthons for the synthesis of biologically active compounds, have been prepared in good yield and with high stereoselectivity through palladium-catalyzed heteroannulation of 2-iodophenol or 2-iodo-N-mesylaniline with enantiomerically pure or enriched α-arylpropargylamines. 相似文献
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Alan R. Katritzky Kenneth A. Heck Jianqing Li Adam Wells Catherine Garot 《合成通讯》2013,43(14):2657-2670
α-Lithiated 1-(1-alkenyl)benzotriazoles, generated from the reactions of 1-(1-alkenyl)benzotriazoles with n-BuLi, react with a variety of electrophiles to afford α-substituted 1-(1-alkenyl)benzotriazoles which undergo epoxidation with m-CPBA followed by hydrolysis to give α-hydroxy ketones in good yields. Thus, 1-(1-alkenyl)benzotriazoles behave as α-hydroxyacyl anion equivalents. 相似文献
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1-chloro-1-alkenyl phenyl sulfides treated with bromine followed by hydrolysis or methanolysis give α-bromo phenyl thiocarboxylic esters and α-phenyl-thio methyl carboxylic esters. Direct oxidative solvolysis with bromine and alcohol give α-bromo alkyl carboxylic esters. 相似文献
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A 520-base pair human IFN-α gene was isolated by PCR method twice from chromosome DNA of a Chinese (Han Nationality) fetal liver. The nucleotide sequences were determined. These two separately amplified DNA fragments shared the completely identical nucleotide sequence but possessed C and G at positions 410 and 541, respectively, which differ from those oflFN-α1 and IFN-αD previously described. Therefore the deduced amino acid sequence would have an Ala at position 114 and a Val at position 158. At all other sites it has the same amino acids as those in IFN-α1 and IFN-αD. We recommend that IFN-αD gene, IFN-αI gene and IFN-αI/158V gene found in our laboratory, be named IFN-αla gene, IFN-αlb gene and IFN-αlc gene. 相似文献
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Colpaert F Mangelinckx S Rocchetti MT De Kimpe N 《Organic & biomolecular chemistry》2011,9(2):549-558
α-Methoxy- and α-ethoxyketones, as important intermediates in organic synthesis and flavor compounds in food chemistry, were synthesized by deprotonation of N-(1-alkoxy-2-propylidene)isopropylamine, prepared by condensation of the corresponding α-alkoxyacetone with isopropylamine, and subsequent reaction of the corresponding 1-azaallylic anions with alkyl halides to afford α'-alkylated, α-alkylated and α,α'-dialkylated ketimines. Hydrolysis of the imino function led to the desired substituted α-alkoxyketones. The ratio of α-, α'-, and α,α'-(di)alkylated compounds depended on the amount of base used and on the nature of the alkylating reagent. 相似文献
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LI Shuo LI Lei XU Peng-Fei 《有机化学》2003,23(Z1):419-419
Optically active nonproteinogenic amino acids[ 1] are valuable compounds of high interest not only owing to their remarkable pharmacological and biological activities, but also for their role as an investigative topographic probe for bioactive conformations of peptides and the mechanisms of enzyme reactions.[2] 相似文献
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《Journal of carbohydrate chemistry》2013,32(1-2):79-88
2,3;5,6-Di-O-isopropylidene-α-d-mannofuranosyl chloride reacted with allylmagnesium bromide with preferential inversion of the anomeric configuration to furnish a mixture of the 1-allyl-1-deoxy-β- and α-d-mannofuranoses. Separation of β and α derivatives was possible only after conversion to the 1-allyl-1-deoxylyxofuranoses 2 and 3. The β configuration of the predominant product 2 was proved using the NOE method. 相似文献
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Zheng Chang XIONG Lu Ling WU Xian HUANGDepartment of Chemistry Zhejiang University Xixi Campus Hangzhou.State key Laboratory of Organometallic Chemistry Shanghai Institute of Organic Chemistry Chinese Academy of Sciences Shanghai . 《中国化学快报》2004,(4)
Hydrozirconation of 1-alkylnylphosphonates gives the organozirconium(Ⅳ) complexes 2 in syn-addition way. Complexs 2 was trapped with NCS, NBS or I2 to afford stereodifined α-halo-1-alkenylphosphonates in moderate to high yields. 相似文献
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K. Boukallaba A. Elachqar A. El Hallaoui A. Alami S. El Hajji B. Labriti 《Phosphorus, sulfur, and silicon and the related elements》2013,188(4):819-823
α-heterocyclic α-aminophosphonates were obtained in good yields by N-of several nitrogen heterocycles with α-azido-α-aminophosphonate 1. 1 相似文献
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Samir Acherar 《Tetrahedron letters》2009,50(46):6377-6379
The preparation of optically pure Nα-Me, Nβ-Boc-protected α-hydrazinoacids in large scale is described via a SN2 protocol. These compounds were used as starting materials for the synthesis of 1:1:1 [Nα-Me α-hydrazino/α/Nα-Me α-hydrazino]trimers. 相似文献
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Summary Many receptors, including 1 adrenergic receptors, have a range of subtypes. This offers possibilities for the development of highly selective antagonists with potentially fewer detrimental effects. Antagonists developed for 1A receptors, for example, would have potential in the treatment of benign prostatic hyperplasia. As part of the molecular design process, structural features necessary for the selective affinity for 1A and 1B adrenergic receptors have been investigated. The molecular modelling software (particularly the Apex module) of Molecular Simulations, Inc. was used to develop pharmacophore models for these two subtypes. Low-energy conformations of a set of known antagonists were used as input, together with a classification of the receptor affinity data. The biophores proposed by the program were evaluated and pharmacophores were proposed. The pharmacophore models were validated by testing the fit of known antagonists, not included in the training set. The critical structural feature for selectivity between the 1A and 1B adrenergic receptor sites is the distance between the basic nitrogen atom and the centre of an aromatic ring system. This will be exploited in the design and synthesis of structurally new selective antagonists for these sites. 相似文献