Synthesis of New Glycerolipids Linked to Hydroxamate Derivatives Designed for Two-Dimensional Crystallization of Aminopeptidase M

The synthesis of glycerolipids linked to hydroxamate derivatives designed for two-dimensional crystallization of aminopeptidase M is reported. The lipid moieties are readily obtained using a convergent pathway. Their structure allows the introduction of a wide variety of ligands of biological interest.     

含铁骨架Fe-Al-EU-1分子筛的设计合成和晶化

以溴化六甲双铵(HMBr2)为模板剂,在HMBr2-Na2O-Al2O3-SiO2-Fe2O3-H2O体系中,采用水热法合成了高结晶度Fe-Al-EU-1分子筛,通过X射线粉末衍射(XRD)、扫描电子显微镜(SEM)、热重-微分热重(TG-DTG)分析、N2吸附-脱附、固体核磁共振(NMR)、紫外-可见(UV-Vis)吸收光谱和X射线吸收谱的精细结构(XAFS)等测试手段对合成样品的物理化学性质、铁在分子筛骨架的成键状态进行表征.结果表明:随着原始溶胶中铁的质量分数增加,Fe-Al-EU-1分子筛的晶胞体积增大;铁掺杂使Al-EU-1分子筛的表面积(BET)从272m2·g-1增加到365m2·g-1;模板剂脱除和分解温度降低;铁离子加入溶胶,导致zeta电位降低,胶体粒子容易聚集,分子筛外形增大.UV-Vis结果显示:由于220-250nm处的分子筛骨架中氧原子的成键2p电子向骨架四配位铁原子的空d轨道产生p-d跃迁,导致其特征峰的吸收峰强度急剧增加,在373nm左右骨架位的四配位铁原子与相邻的硅氧基团配位键合,产生能级分裂的d-d电荷跃迁峰且峰强度增加.XAFS结果表明:随着晶化过程的进行,边前1s→3d吸收峰和1s→4p主吸收峰发生了明显变化,原始溶胶样品在形成四配位铁物种结构单元后,逐步转化形成四面体配位的铁-硅-氧骨架铁物种,铁-硅-氧离子键结构单元也随之转变为四面体配位共价键结构的骨架铁物种.     

Synthesis and Anticancer Activity of New Substituted Piperidinones Linked to Pyrimidine,Thiazole, and Triazole Glycoside Derivatives

Russian Journal of General Chemistry - New piperidinone incorporating pyrimidine, triazine, diazipine, oxatriazine, and thiazole derivatives have been synthesized starting with...     

Synthesis and Anticancer Activity of 1,2,4-Oxadiazol Linked Benzimidazole Derivatives

Russian Journal of General Chemistry - A new series of 1,2,4-oxadiazole linked benzimidazole derivatives 11a–11j are synthesized. Their structures are confirmed by 1H and 13C NMR and mass...     

Synthesis,Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives

A new series of 5‐fluoro‐N⁴‐(3‐(4‐substitutedbenzylamino)phenyl)‐N²‐(4‐morpholinophenyl)pyrimidine‐2,4‐diamine derivatives ( 7a , 7b , 7c , 7d , 7e , 7f , 7g , 7h , 7i , 7j ) are prepared from using an intermediate compound 5‐fluoro‐N⁴‐(3‐(aminophenyl)‐N²‐(4‐morpholinophenyl)pyrimidine‐2,4‐diamine ( 5 ). The structures of the newly synthesized products are established from their spectral ¹H‐NMR, ¹³C‐NMR, ¹⁹F‐NMR, ESI‐MS, and analytical data. Here we report the synthesized compounds and larvicidal activity. All the compounds are screened for their significant larvicidal activity against third instar larvae at 24, 48, and 78‐h time exposure, and values were compared with standard drug Malathion. The Compounds 7i , 7a , 7c , 7f , and 7j exhibited significant activity. However the compounds 7b , 7e , 7d , and 7h showed excellent activity when compared to the above compounds and to standard drug malathion too because of the presence of mild electron withdrawing groups such as trifluoro, fluorine, hydroxy, nitro, and methoxy derivatives which are attached to the benzyl ring.     

Synthesis and Insecticidal Activity of Tetrazole‐Linked Triazole Derivatives

A new series of 4‐(4‐substitutedbenzylideneamino)‐5‐((1‐methyl‐1H‐tetrazol‐5‐ylthio)methyl)‐4H‐1,2,4‐triazole‐3‐thiol derivatives ( 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h , 5i , 5j , 5k ) are prepared using 4‐amino‐5‐((1‐methyl‐1H‐tetrazol‐5‐ylthio)methyl‐4H‐1,2,4‐triazole‐3‐thiol ( 4 ), as an intermediate compound. The structures of all the newly synthesized products are established supported by their spectral ¹H NMR, ¹³C NMR, FTIR, electrospray ionization mass spectrometry (mass), and analytical data. All the compounds are screened for their insecticidal activity against Plodia interpunctella, and six compounds exhibited significant activity.     

New Possibilies of Glycerophosphocycles in the Synthesis of Phospholipids

Abstract

The reaction of cycloamidophosphites and cyclophosphites of glycerol with halogenamides of organic acids was studied.     

Synthesis and Characterization of a Novel Class of PPV Derivatives Covalently Linked to C60

Poly(phenylenevinylene) (PPV) derivatives covalently linked to fullerene C₆₀ (PPV‐1‐C₆₀ and PPV‐2‐C₆₀) were synthesized by cycloaddition reaction between C₆₀ and azide group‐containing PPV derivatives. By tuning the initial feed ratio of the azido monomer, the content of C₆₀ in the copolymers was controlled. The copolymers were partially soluble in common organic solvents and were characterized by means of ¹H NMR, FT‐IR, UV‐Vis and fluorescence spectroscopy, as well as by GPC, TGA and cyclic voltammetry techniques.     

Synthesis of New Quinoline Derivatives

The synthesis of some new functionalized quinolyl derivatives has been described, based on the 1,3‐dipolar cycloaddition of an azomethine ylide, generated from sarcosine or N‐benzylglycine and paraformaldehyde, to 2‐chloro‐3‐quinolinecarbaldehydes.     

Substituted 4,5-Dihydrooxazoles in the Synthesis of New Phospholipids

Russian Journal of Organic Chemistry -     

Synthesis of New Benzoimidazole Derivatives

The reactions of cryptotanshinone and tanshinone llA with cadaverine and putrescine were investigated. Six new compounds, four with imidazole functional groups and two with oxazole groups, were obtained. The possible reaction mechanism was proposed.     

Synthesis of New Aminophosphonothiophene Derivatives

The reaction of n , n '-diphosphonylketones 1 with active methylenenitriles and sulfur in basic conditions led to the new 5-amino-2-(phosphonomethyl)-3-(phosphonoethyl)thiophenes 2 . These compounds were then used in the Horner-Wadsworth-Emmons reaction to give 5-amino-2-alkenyl-3-(phosphonoethyl)thiophenes 3 . The structure of all obtained products was confirmed by NMR ( 1 H, 31 P, 13 C) and IR spectroscopy.     

Synthesis of New Quinoxaline Derivatives

New quinoxaline derivatives were prepared by the reaction of 2-hydroxyquinoxaline 1 and alkyl or alkylaminoalkyl halides in dimethylformamide using potassium carbonate as a base. The hydroxyl group was readily converted into a thiol function by treatment with phosphorus pentasulfide and/or Lawesson's reagent in pyridine, and the subsequent alkylation of the thiol group was carried out under phase-transfer catalyst conditions. Chlorination of 1 was carried out with phosphorus oxychloride. Branching of alkylamino side chains to the 2-OH, 2-SH, and 2-Cl quinoxalines resulted in the synthesis of several compounds. Synthesis and alkylation of 2-hydroxy 7-nitroquinoxaline are also reported.      

Synthesis of Isomeric Dimers of Deoxycholic Acid Derivatives Linked by 1,2,3-Triazole

Steroidal propargylic ester 6 and the propiolic ester 7 were prepared in a few steps from the deoxycholic acid. The Huisgen cycloaddition reaction of alkynes 6 and 7 as dipolarophiles with a 1,3-dipolar compound, the azide 5, afforded the dimeric compounds 8 and 9, respectively, in good yield. The dimers of deoxycholic acid derivatives linked by 1,4-disubstituted 1,2,3-triazole were characterized by spectroscopic methods.     

Efficient Synthesis of Unsaturated 1-Monoacyl Glycerols for in meso Crystallization of Membrane Proteins

A highly efficient synthesis of unsaturated 1-monoacyl glycerols was established to fulfill the pressing need for materials that form lipidic mesophases utilized in membrane protein crystallization.     

Studies on the Synthesis and Structure of New Urea‐Linked Sugar Podando‐Coronand Derivatives

With the aim to develop direct, simple, and efficient coupling procedures involving saccharides and cyclodextrins (CDs), the modified Staudinger method, the phosphine imide method, was chosen as a promising versatile way to reach the goals. Thus, the new cyclam derivatives 6 – 9 were obtained in good yields (see Scheme). In the case of β‐cyclodextrin, the method also allowed the synthesis of the icosa‐O‐acetyl‐6^A‐isocyanato‐6^A‐deoxy‐β‐CD sugar isocyanate 11 and of symmetrical or unsymmetrical carbohydrate carbodiimides 12 and 17 under smooth conditions and in a simple way. Structural, theoretical, and experimental investigations on several urea‐like cyclams revealed the fundamental role played by permanent strong H‐bonds between urea functions in the conformational equilibrium of the molecules.     

Synthesis and Anticancer Evaluation of Amide Derivatives of 1,3,4-Oxadiazole Linked with Benzoxazole

Russian Journal of General Chemistry - A novel series of amide 1,3,4-oxadiazole linked benzoxazole derivatives 12a–12j are synthesized and their anticancer activity is screened against four...     

Synthesis of Defective Phospholipids

Phospholipids have been synthesized that possess a normal 16-carbon chain plus a "defective" chain only 8 or 12 carbons long and terminated with methoxyl, hydroxyl, or carboxyl groups. In addition, dimeric phospholipids have been prepared in which two phospholipid units are joined at position-1 with chains of 22 or 32 carbons while unconnected chains at position-2 are, once again, short and functionalized. These phospholipids are potentially useful for constructing membranes that contain cavities or irregularities and, therefore, are capable of serving as self-assembled host systems in which drugs and other guest molecules are retained and, perhaps, eventually released.