Studies on 1, 2, 4-Benzothiadiazine 1, 1-Dioxide IX.1 Synthesis and Pharmacological Evaluation of 1, 2, 4-Benzothiadiazine 1, 1-Dioxide Biphenyl Tetrazoles as Angiotensin II Antagonists

In the course of our investigations on the development of cardiovascular agents, 3-butyl-2-[2′-(2H-tetrazol-5-yl)bipheny]-4-yl]methyl-2H-1, 2, 4-benzothiadiazine 1, 1-dioxide ( 2 ) was considered as a potential angiotensin II antagonist on the basis of bioisosteric replacement of the quinazoline ring of compound 1 with a 1, 2, 4-benzothiadiazine 1, 1-dioxide ring system. Alkylation of 6 with 4 afforded 7 and 8 in 24% and 28% yields, respectively. An attempt to remove the trityl group of compounds 7 and 8 under acidic condition gave the ring opened products 9 and 11 in 28% and 36% yields, respectively. However, compounds 2 and 10 were obtained in 46% and 85% yields when compounds 7 and 8 were refluxed in methanol. Preliminary assays of compounds 9 and 11 against angiotensin II receptors revealed weak activity with IC₅₀ values of 3.6 μM and 5.4 μM, respectively. Compound 10 (IC₅₀ = 87 nM) exhibited stronger binding affinity than compound 2 (IC₅₀ = 750 nM).     

Novel reaction of 1-aryl-2-bromodiazene 1-oxides with olefins. Synthesis of 1-aryl-2-(2-bromoalkyl)diazene 1-oxides

The addition of 1-aryl-2-bromodiazene 1-oxides to olefins yields 1-aryl-2-(2-bromoalkyl)diazene 1-oxides (4). A radical mechanism of the reaction has been suggested. Compounds4 decompose to give bromohydrazones of formaldehyde and aldehydes. The structural factors that affect the rate of this process are discussed.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 917–923, May, 1995.The work was carried out in the Scientific Educational Center of the Institute of Organic Chemistry of the RAS with financial support of the Russian Foundation for Basic Research (Project No. 93-03-18461).     

ChemInform Abstract: The Gallides SrRh2Ga2, SrIr2Ga2, and Sr3Ir4Ga4.

The title gallides are prepared from the elements by induction melting and subsequent annealing (Ta ampules, 800 mbar Ar, 873—1073 K, 4 d) and characterized by powder and single crystal XRD.     

ChemInform Abstract: Exotic Structures of Si2B2H4.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

Über N1- und N2-substituierte 2-Amino-5,6-dihydro-4(1H)-pyrimidinone

The reactions of the monosubstituted guanidines2 b-h with methyl acrylate in dimethylformamide or ethanol as solvent preferentially afford 1-substituted 2-amino-5,6-dihydro-4(1H)-pyrimidinones6 b-h. The structures of 1-hexyl- and 1-benzyl-4-pyrimidinones6 c, e and of the picrate of 1-phenylpyrimidinone6 g were proved by comparison with authentic samples, which were prepared from N-substituted ethyl 3-amino-propionates14 c, e andg and cyanamide. Accordingly,6 g is not identical with authentic 2-phenylaminopyrimidinone7 g (prepared from 2-methylthio-4-pyrimidinone10 and 2-thioxo-4-pyrimidinone12 respectively, compare¹⁰).N,N-Disubstituted guanidines2 i-m react with methyl acrylate in dimethylformamide as solvent to afford N²,N²-disubstituted 2-amino-5,6-dihydro-4-(1H)-pyrimidinones7 i-m. Action of morpholine-4-carboxamidine (21) on methyl acrylate in ethanol yields 2-morpholinopyrimidinone71 as byproduct and 3-ethoxy-N-[morpholino(amino)methylene]propionamide (91) as mainproduct.

Herrn Prof. Dr.Robert Ott mit den besten Wünschen zum 60. Geburtstag gewidmet.     

ChemInform Abstract: Crystal Structure and Spectroscopic Studies of LiNH4(H2PO4)2 — A New Solid Acid in the LiH2PO4—NH4H2PO4 System.

LiNH₄(H₂PO₄)₂ is prepared from an equimolar aqueous mixture of NH₄H₂PO₄ and LiH₂PO₄ by slow evaporation at 25 °C.     

ChemInform Abstract: α-Ammonium Vanadium Hydrogen Phosphate, α-(NH4)V(HPO4)2.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

Beiträge zur Chemie des Phosphors. 245 [1], LiP7(BNEt2)2 und P7(BNEt2)4Cl: Zwei neuartige polycyclische Boraphosphane

Contributions to the Chemistry of Phosphorus. 245, LiP₇(BNEt₂)₂ and P₇(BNEt₂)₄Cl: Two Novel Polycyclic Boraphosphanes The directed synthesis of a noval tetracyclic heteropolyphosphane skeleton from a tricyclophosphane has been achieved by condensation of Li₃P₇ · 3DME with Cl(Et₂N)B‐B(NEt₂)Cl to the diboranonaphosphanide LiP₇(BNEt₂)₂ ( 1 ). When the reaction proceeds the mixed‐substituted diboranonaphosphane P₇(BNEt₂)₄Cl ( 2 ) is formed. According to their ³¹P NMR spectra 1 and 2 possess a B₂P₇(3) skeleton analogous to that of the hydrocarbon deltacyclane. Additional weak signals in the ³¹P NMR spectrum of 2 indicate that also small amounts of the symmetrically substituted diborane(4) P₁₄B₆(NEt₂)₆ ( 3 ) are formed.     

ChemInform Abstract: Pseudopotential Investigations on the Molecules Cu2Si2, Cu2Sn2, Cu4Si4, and Cu4Sn4

show the equilibrium structures to be the butterfly arrangement for the Cu₂X₂ clusters and the heterocubane arrangement for the Cu₄X₄ clusters.     

Ternäre Nickelphosphide und -arsenide mit einem Metall: Nichtmetall-Verhältnis von 2:1

Ternary Phosphides and Arsenides of Nickel with a Metal: Non-Metal Ratio of 2:1 Several new ternary phosphides and arsenides of nickel were prepared by reaction of the elements. SrNi₅P₃, SrNi₅As₃, and EuNi₅As₃ crystallize in the LaCo₅P₃ structure with the following lattice constants [Å]: BaNi₉P₅ (a = 6.534(1) Å, c = 10.847(2) Å) and BaNi₉As₅ (a = 6.760(1) Å, c = 11.226(2) Å) crystallize in a new type of structure (P6₃/mmc, Z = 2). The characteristic polyhedra are trigonal Ni-antiprisms centered by P or As atoms and trigonal Ni-prisms with vacant centres and sides capped by non-metal atoms. U₂Ni₁₂P₇ (a = 9.077(2) Å, c = 3.694(1) Å) has a Zr₂Fe₁₂P₇ structure (P6 , Z = 1).     

Na2CrO4-(NH4)2CrO4-H2O体系的相图

铬盐工业是无机盐工业的一个主要分支,其主要产品有重铬酸钠、铬酸酐、铬酸铵、氧化铬等,广泛用于合金材料、电镀、制革、印染、橡胶等部门,是国民经济中重要的基础化工原料工业．铬盐生产系先将铬铁矿制成铬酸钠及重铬酸钠,然后再进一步加工制成其它铬盐产品．在铬盐...     

β-甲萘醌催化氧化合成技术研究进展

综述了不同原料合成K系维生素重要中间体β-甲萘醌的不同方法及相应催化氧化体系建立的研究进展。与传统工业生产工艺相比较,着重分析以β-甲基萘为原料所采用的各催化剂类别及其催化氧化合成路线的特点和不足;结合国内外催化材料使用和国内生产现状,提出环境友好绿色催化氧化合成β-甲萘醌的未来发展趋势及研究方向。