- A new family of water-soluble, third generation antitumor platinum complexes
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[1,1-Cyclobutanedicarboxylato(2-)-0,0'](1,3-dioxane-5,5-dimethanamine- ,N')platinum (II), 3a, a third generation, very water-soluble platinum complex, has been synthesized along with several of its analogues. All members of the new family contain a 1,3-dioxane or 1,3-dioxolane-1,3-diamine as their basic ligand, a moiety which contributes to their increased water solubility, and a bidentate acid ligand, which is responsible for their good stability. They were all easily crystallized and characterized by 1H NMR and elemental analysis, and the parent complex 3a was further characterized by 13C NMR. Their very desirable physical properties combined with their broad spectrum of antitumor activity and reduced toxicity make them good candidates in further development.
- Bitha,Carvajal,Citarella,Delos Santos,Durr,Hlavka,Lang Jr.,Lindsay,Thomas,Wallace,Lin
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- ERK INHIBITOR AND USE THEREOF
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Disclosed are a compound (as shown in formula I) as an extracellular signal-regulated kinase (ERK) inhibitor, a pharmaceutical composition thereof, a preparation method therefor, and use thereof in treating ERK-mediated diseases. Said compound plays a role by regulating a plurality of processes such as cell proliferation, apoptosis, migration and angiogenesis.
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Paragraph 0101-0102
(2021/04/16)
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- Diverse ring opening of thietanes and other cyclic sulfides: An electrophilic aryne activation approach
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Organosulfides are a common class of structure units in bioactive molecules and functional materials motivating continuous developments of efficient synthetic methods. Herein, we report an electrophilic aryne-activated ring opening protocol of one or two
- Zheng, Tianyu,Tan, Jiajing,Fan, Rong,Su, Shuaisong,Liu, Binbin,Tan, Chen,Xu, Kun
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supporting information
p. 1303 - 1306
(2018/02/14)
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- METHOD FOR PREPARING LIGAND FOR POLYKETONE POLYMERIZATION CATALYST
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The present disclosure provides a method for preparing ((2,2-dimethyl-1,3-dioxane-5,5-diyl)bis(methylene))bis(bis(2-methoxyphenyl)phosphine), a ligand for a polyketone polymerization catalyst, under mild conditions with high purity and high yield. Therefore, the preparation method of the present disclosure can be easily applied to mass production.
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Paragraph 48; 49; 50
(2017/07/06)
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- POLYKETONE POLYMERIZATION CATALYST
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Provided are a novel polyketone polymerization catalyst and a method of preparing a ligand, which can reduce production costs and can enable commercial mass synthesis by using ((2,2-dimethyl-1,3-dioxane-5,5-diyl)bis(methylene))bis(bis(2-methoxyphenyl)phosphine) as a ligand constituting the polykeytone polymerization catalyst, the ligand having a simple structure and a small molecular weight while having high activity.
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Paragraph 0042; 0043; 0044; 0045; 0046
(2016/12/01)
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- The influence of OH groups in [Fe(CO)3]2[(μ- ECH2)2C(CH2OH)2] (E = S, Se) complexes toward the cathodic process
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[FeFe] hydrogenase model complexes [Fe(CO)3]2[(μ- ECH2)2C(CH2OH)2] (E = S (1) or Se (2)) containing CH2OH bridgehead substituents were synthesized via reaction of equimolar amounts of 4, 4-bis(hydroxymethyl)-1, 2-dithiolane (A) or 4, 4-bis(hydroxymethyl)-1, 2-diselenolane (B) with Fe3(CO) 12 in toluene at 100°C. The presence of OH groups in complexes 1 and 2 is found to influence the cathodic processes and their potentials. The catalytic reduction of acetic acid (AcOH) occurs by the anions 1- and 2-, while the neutral complexes are procatalysts. Copyright
- Trautwein, Ralf,Almazahreh, Laith R.,Goerls, Helmar,Weigand, Wolfgang
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p. 1512 - 1519
(2013/08/23)
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- Host-guest complexes of cucurbit[8]uril with some pentaerythritol derivative guests
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A series of first generation dendritic guests from pentaerythritol derivatives have been designed and synthesized. Investigation of the complex structures of cucurbit[8]uril (Q[8]) and the guests based on the 1H NMR technique have revealed that the host Q[8] selectively included different branch(es) of the first generation dendritic guests and formed inclusion complexes with different structural conformations. The experimental results obtained from electronic absorption spectroscopy showed that the 1:1 ratio of Q[8]-based host-guest inclusion complexes have moderate stability with an average formation constants of 104 L mol-1. The single crystal structures of some of the guests (g5 and g6) and Q[8]-guest complexes (Q[8]-g4 and Q[8]-g6) further confirm but in some cases contradict the research results of the 1H NMR technique and electronic absorption spectroscopy in aqueous solution. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2011.
- Li, Xian-Mei,Fan, Fan,Lu, Jing-Song,Xue, Sai-Feng,Zhang, Yun-Qian,Zhu, Qian-Jiang,Tao, Zhu,Lawrance, Geofferey A.,Wei, Gang
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p. 1088 - 1095
(2011/07/08)
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- Synthesis and characterisation of 2,2-bis(hydroxymethyl)-1,3-diselenolato metal(II) complexes bearing various phosphanes
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An improved synthesis of 4,4-bis(hydroxymethyl)-1,2-diselenolane and the complexation properties of the corresponding diselenolato dianion to group-10 metals are reported. We describe an efficient and straightforward procedure that bypasses the isolation of the malodorous and airsensitive diselenol and starts with the diselenide appropriate group-10 metal complex bearing phosphane and chlorido ligands. A series of complexes with various monoand bidentate phosphanes is prepared and characterised by multinuclear NMR spectroscopy, mass spectrometry, and elemental analysis. Furthermore, the structure of most complexes is studied by single-crystal X-ray diffraction to establish their supramolecular arrangement in the solid state. Consequently, several group-10 metal complexes with P-M-P angles (bite angles) in the range from 71-108° are investigated. The use of the sterically demanding bridging phosphane 4,5-bis(diphenylphosphanyl)-9,9-dimethylxanthene, which exhibits a large bite angle yields a mixture of a di- and trinuclear complex. While the platinum-containing complexes are proven to be rather stable, the palladium and nickel analogues tend to decompose. Especially, the nickel complexes were found to be sensitive against: oxidation. This circumstance leads to the formation of the so far unknown 1,8-bis(diphenylphosphanyl)naphthalene monooxide, the formation and structure of which could be confirmed from NMR spectroscopic data and single-crystal X-ray diffraction.
- Niksch, Tobias,Goerls, Helmar,Friedrich, Manfred,Oilunkaniemi, Raija,Laitinen, Risto,Weigand, Wolfgang
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scheme or table
p. 74 - 94
(2010/04/01)
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- MACROCYCLIC INDOLE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C INFECTIONS
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A class of macrocyclic compounds of formula (I), wherein R7, R9, B, F, M, Q, W, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also p
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Page/Page column 69
(2009/03/07)
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- NOVEL PHOSPHODI ESTERASE INHIBITORS
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The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further re
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Page/Page column 48
(2008/12/08)
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- PENTACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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Page/Page column 27
(2008/06/13)
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- Synthesis of thietane nucleosides by glycosidation of thietanose derivatives with nucleobases
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Thietane nucleosides were synthesized by the glycosidation of glycosyl fluoride with nucleobase.
- Nishizono, Naozumi,Sugo, Michiyasu,Machida, Minoru,Oda, Kazuaki
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p. 11622 - 11625
(2008/03/13)
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- Nucleosides and nucleotides. 159. Synthesis of thietane nucleosides via the Pummerer reaction as a key step
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New thymine thietane nucleosides 7 and 20 were synthesized via Pummerer rearrangement of the corresponding sulfoxides 5 and 18 in the presence of thymine. TMSOTf, Et3N, and ZnI2 as a key step.
- Nishizono, Naozumi,Koike, Nobuaki,Yamagata, Yuriko,Fujii, Satoshi,Matsuda, Akira
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p. 7569 - 7572
(2007/10/03)
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- Process for preparing azetidine derivatives and intermediates thereof
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The invention provides a process for preparing azetidine-3-carboxylic acid or salts thereof; useful as chemical hybridizing agents, which comprises treating a compound of the formula STR1 wherein R represents a hydrogen atom or a group of formula R1 R2 CH-- wherein R1 and R2 are independently selected from hydrogen, alkyl or optionally substituted phenyl moieties, with nitric acid and subjecting the resulting initial product to acid conditions to produce an acid-addition salt of azetidine-3-carboxylic acid, and thereafter, if desired, converting the acid-addition salt to the free acid or another salt of the acid, 1-nitrosoazetidine-3,3-dicarboxylic acid, 1-nitrosoazetidine-3-carboxylic acid and salts thereof being intermediates in the process.
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- Azetidine derivative
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2-Benzyl-7,7-dimethyl-6,8-dioxa-2-aza-spiro[3,5]nonane of the formula STR1 and a process for the preparation of that compound, which compound is useful as an intermediate in the preparation of 3-carboxy azetidine.
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- Process for preparation of (poly)cyclic polyethers
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In the preparation of (poly)cyclic polyethers by a cyclic Williamson synthesis, the improvement of contacting the reactants in a hindered (C4 -C14) alkanol. For example, bis-chloroethyl ether and the disodium salt of tetraethylene glycol are contacted in t-butanol to produce the cyclic polyether STR1 in high yields.
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