- Microwave-assisted oxidation of indan-1-ones into ninhydrins
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A simple and general microwave-assisted selenium oxidation has been developed for the synthesis of substituted ninhydrins from indan-1-ones in order to access to indeno[1,2-b]indoles substituted on the A ring. This efficient and convenient oxidation, using selenium dioxide under microwave irradiations, afforded mono- and di-substituted ninhydrins in a single step reaction with good yields.
- Marminon, Christelle,Nacereddine, Abdelhamid,Bouaziz, Zouhair,Nebois, Pascal,Jose, Joachim,Le Borgne, Marc
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supporting information
p. 1840 - 1842
(2015/03/30)
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- Facile synthesis of 1,2,3-tricarbonyls from 1,3-dicarbonyls mediated by cerium(IV) ammonium nitrate
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A mild and efficient protocol for the synthesis of vicinal tricarbonyl compounds from β-dicarbonyls in a single step using cerium(IV) ammonium nitrate as a catalytic oxidant is described. Ease of execution, wide substrate scope and the suitability for the synthesis of commercially important compounds like ninhydrin, alloxan and oxoline make this reaction particularly noteworthy.
- Sivan, Akhil,Deepthi, Ani
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supporting information
p. 1890 - 1893
(2014/03/21)
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- PAR4 AGONIST PEPTIDES
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The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.
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Page/Page column
(2013/11/06)
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- DIVERGENT SYNTHESIS OF LOOPED POLY(ESTER)-AND POLY(ETHER)-SUBSTITUTED DENDRONS AND DENDRIMERS
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The present invention describes a process for preparing new looped dendrimer and dendron compounds by controlling the molar amount of branch cell reagent monomer that is combined with various cores bearing core-XR functionalities (e.g., primary, or secondary amines, thiol, or epoxy functionalities). These looped, macrocyclic structures are more robust to various conditions, with greater resistance to acid/base hydrolysis. Alternatively, the looped, macrocyclic structure may offer new orientations that would qualify it as a better chelation ligand for metals, and other similar uses.
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- Solid Support for Fmoc-Solid Phase Synthesis of Peptides
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The present invention provides compositions and processes for the solid phase synthesis of polypeptides. In particular, the present invention provides solid supports and processes for preparing solid supports for the synthesis of polypeptides.
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- Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation
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The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
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- Method of inhibiting nonspecific interaction between molecules on solid phase support
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The present invention provides a method of suppressing the nonspecific interaction between molecules, characterized in that in a process to immobilize a molecule onto a solid phase carrier and analyze the specific interaction between the molecule and a molecule that specifically interacts with the molecule on the solid phase, the hydrophobic property of the solid phase surface in the solid phase carrier is regulated, particularly a hydrophilic spacer is interlaid at the time of immobilization of the molecule onto the solid phase carrier, which method makes it possible to suppress the nonspecific interaction between the molecules, and to reduce nonspecific adsorption to the solid phase.
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- Chemistry of Free Cyclic Vicinal Tricarbonyl Compounds ('1,2,3-Triones'). Part 3. Polar and Redox Reactions of 1,2,3-Triones with Enamines of Different Types - News on Oxonol Dyes, Radicals, and Biradicals
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The central C=O groups of cyclic 1,2,3-triones possess outstanding electrophilic (electron-pair-accepting) as well as oxidizing (one-electron-accepting) properties. Thus, 1,2,3-triones are chemically related to 1,2- and 1,4-benzoquinones. Whereas polar reactions with carbanion-like (electron rich) species give rise to nucleophilic addition reactions to C=O groups under exclusive C,C-bond formation, SET (single-electron transfer) or redox reactions effect a partial 'carbonyl Umpolung' via ketyl intermediates (C,C- and/or C,O-bond formation). Here, we report on numerous reactions between electron-rich, more- or less-polar enamines with 5,5-dimethylcyclohexane-1,2,3-trione (9a) and 1H-indene-1,2,3-trione (9b). Various new derivatives of basic oxonol dyes were formed, including the first oxonol dye incorporating a 1,3-dioxocyclohexyl moiety. A novel stable radical, 50/50′, was obtained from 9b and lla via addition, hydrolysis, and treatment with conc. H2SO4. Radical 50/50′ represents a vinylogous 'monodehydroreductone' and is, thus, related to monodehydroascorbic acid (143), to Russell's radical cation (144), to indigo (141/141′), and to quinhydrone.
- Schank, Kurt,Lieder, Robert,Lick, Carlo,Glock, Rebecca
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p. 869 - 924
(2007/10/03)
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- Treatment of obesity
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A method for the treatment of obesity in an animal such as a human, comprises administering to the animal an effective amount of a peptide which comprises an analogue of the carboxyl-terminal sequence of a growth hormone, particularly an analogue of the carboxyl-terminal sequence of human growth hormone containing amino acid residues 177-191. A pharmaceutical composition for use in the treatment of obesity is also disclosed.
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- ARYL AND BIARYL COMPOUNDS HAVING MCH MODULATORY ACTIVITY
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In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor. An illustrative inventive compound is shown below:
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- SOLUBLE COMBINATORIAL LIBRARIES
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The present invention relates to novel soluble combinatorial libraries, comprising a soluble phase in solution attached to a core molecule, and allowing the improved high-yield and efficient production of soluble combinatorial libraries. Some specific examples of the soluble combinatorial libraries claimed herein comprise one or more of the following: amino acids, α-azetide amino acids, triazine dione molecules, γ-lactamtide molecules, δ-lactamthiotide molecules, β-lactam nucleus containing molecules, lycoramine alkaloid nucleus containing molecules, and β-blocker nucleus molecules. Further, a split synthesis technique for generating libraries of combinatorial molecules employs a biphasic macromolecular support which is soluble during the pooling, splitting, and coupling steps but which is insoluble during the washing step. The use of a biphasic macromolecular support in its soluble phase significantly enhances the efficiency and performance of the pooling, splitting, and coupling steps. The use of a biphasic macromolecular support in its insoluble phase significantly enhances the efficiency and performance of the washing step.
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- Novel compositions for the delivery of negatively charged molecules
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This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAs, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.
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- Quinolizinones as integrin inhibitors
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The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly αIIbβ3 or αv integrins such as αvβ3 and αvβ5. One embodiment of the present invention comprises a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt, solvate, or metabolic precursor thereof. R1, R2, R3, and R4 are defined herein.
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- Compositions for the delivery of negatively charged molecules
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This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.
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- Nitric oxide synthase inhibitors
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The present invention relates to novel amidino compound of formula (I). to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.
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- Method of detection of influenza virus and compounds for use therein
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The invention provides a method of detection of influenza virus which utilizes compounds able to bind specifically to the active site of influenza virus neuraminidase, and novel compounds for use in the method.
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- Biodegradable contrast media for MR imaging
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A macromolecular contrast agent for magnetic resonance imaging of the vascular system is constructed of a polymeric backbone structure with a plurality of spacer arms bonded to the backbone structure, each spacer arm terminating in at least one paramagnetic complex. The polymeric backbone thus serves as an amplifier by supporting a multitude of paramagnetic complexes, and the spacer arms contribute to the molecular weight. The spacer arms further contribute useful properties to the agent, such as hydrophilicity and the ability to cleave at a relatively rapid rate in blood.
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- Diagnostic/therapeutic agents having microbubbles coupled to one or more vectors
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Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, having reporters comprising gas-filled microbubbles stabilised by monolayers of film-forming surfactants, the reporter being coupled or linked to at least one vector.
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- INHIBITORS OF FACTOR XA
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor xa in vitro or as a therapeutic agent for the prevention and treatment of conditions characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.
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- L-aspartyl-L-thienylalanine methyl ester, process for its preparation and use as sweetener
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L-aspartyl-L-thienylalanine methyl esters of the formula STR1 where A is a radical of the formula STR2 in which R can be H or CH3, a process for its preparation, and its use as sweetener.
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- INHIBITORS OF FACTOR XA
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor Xa in vitro or as a therapeutic agent for the prevention and treatment of conditions: characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.
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- Low molecular weight peptidomimetic growth hormone secretagogues
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The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this invention are used to promote growth in mammals either alone or in combination with other growth promoting compounds, especially IGF-1. In a method of this invention GHRP's in combination with IGF-1 are used to treat Type II diabetes. An exemplary compound of this invention is provided below. STR1
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- Matrix-supported sapphyrins
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The invention relates to the field of polymer- and other matrix-supported sapphyrins. Disclosed are silica gel, glass, resin and other polymer- and matrix-supported sapphyrins and sapphyrin-containing chromatographic and electrophoretic supports.
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- The Hydration of 1,2,3-Indanetriones and Related Triones
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A series of 5-mono- and 5,6-di-substituted 1,2,3-indanetriones, 1,2,3(2H)-phenalenetrione and 1,3-diphenyl-1,2,3-propanetrione have been shown to form 2,2-dihydroxy-1,3-dione hydrates.The rates for the uncatalysed hydrations has been measured at three temperatures and activation paramaters evaluated.The kinetic role of water and solvent isotope effects have been studied.The Hammett reaction constant, ρ, for the uncatalysed hydration of the substituted 1,2,3-indanetriones in 96.7percent (v/v) dioxane-water at 25 deg C was found to be ca. 1.05.The structure of the transition state for the hydration has been discussed and shown to involve two molecules of water, one acting as a nucleophile and the other as a general acid-base catalyst transferring protons.
- Bowden, Keith,Rumpal, Sanjay
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p. 355 - 374
(2007/10/03)
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- METHIONINE SULFONE AND S-SUBSTITUTED CYSTEINE SULFONE DERIVATIVES AS ENZYME INHIBITORS
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This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
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- Cyclic analogs of alpha-MSH fragments
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Cyclic Alpha-MSH fragment analogues of Ac-Nle4 -Glu5 -His6 -D-Phe7 -Arg8 -Try9 -Gly10 -NH2. The method of stimulating melanocytes by the transdermal application of these biologically-active analogues and compositions comprising these analogues for use in the method are disclosed.
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- Nucleoside derivatives
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A nucleoside derivative of formula (1), characterized in that: Y is H or OH or a protected hydroxy group; X is H, a phosphonate group or a phosphoramidite group of formula (II), where R1 and R2 are the same or different, and are selected from alkyl and substituted alkyl, which may be branched or unbranched; and Q is a phosphate protecting group; Z is H, a phosphate or triphosphate group or hydroxy protecting group; X' is a C1-15 alkyl group which may be branched or unbranched; R is an amino protecting group or a fluorophore, or other non-radioactive detectable marker; or the group Y'NHA, where Y' is an alkyl (C1-40) carbonyl group which may be branched or unbranched, and A is an amino protecting group or a fluorophore or other non-radioactive detectable marker. Methods for the synthesis and sequencing of polynucleotides utilizing compounds of formula (I).
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- Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
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This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
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- Amine preparation
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A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-α-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: STR1 wherein R, R1, R2 and R3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.
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- A new synthesis of ninhydrin and its ketals using iodobenzene diacetate
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The oxidation of indene-1,3-dione (2) with iodobenzene diacetate-ROH-H2SO4, followed by the acid hydrolysis of the resulting 2,2-dialkoxyindane-1,3-diones (3), provides a new and convenient method for the synthesis of ninhydrin and its ketals.
- Prakash, Om,Sharma, Pawan K.,Saini, Neena
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p. 632 - 633
(2007/10/03)
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- Chrysospermins, active peptides from apiocrea chrysosperma having a pharmacological effect and a use thereof
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The invention relates to the chrysospermin active peptides of the formula I in which x and y, independently of each other, denote Aib or Iva, which are synthesized by the fungus Apiocrea chrysosperma during fermentation and which accumulate in the culture broth, to a preparation process, to the use of the chrysospermins as pharmacological active compounds, in particular as active compounds against bacteria, fungi and/or nematodes, and for the treatment of rejection reactions in organ transplantations and of tumor disorders, and to the microorganism Apiocrea chrysosperma DSM 7444.
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- Sapphyrin derivatives and conjugates
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The present invention provides various covalently modified sapphyrin derivatives and conjugates, and also, polymers including sapphyrin or derivatives thereof. Disclosed are water soluble sapphyrins, including polyhydroxysapphyrins and sapphyrin-sugar derivatives; sapphyrin-metal chelating conjugates; sapphyrin nucleobase conjugates; and polymer supported sapphyrins. Novel sapphyrin dimers, trimers, oligomers and polymers are also described, which polymers may include repeating units of sapphyrin or sapphyrin derivatives alone, or may further incorporate other units such as nucleobases.
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- Resin for solid-phase peptide synthesis and methods of making it
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The present invention pertains to polyethylene glycol (PEG) derivatized graft supports, to methods for making these supports and to methods of using the supports to synthesize peptides by solid-phase synthesis techniques. The PEG-graft supports of this invention comprise functionalized PEG derivatives which are covalently attached to solid supports, such as polystyrene.
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- Fibrinogen receptor antagonists
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A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
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- Azido-substituted aromatic amino acids
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Azido-substituted aromatic amino acids represented by the following formula I are synthesized through the use of tyrosine phenol-lyase. The azido derivatives are suitable for use as photoaffinity labels and inhibitors; STR1 wherein R1 represents a lower alkyl, a lower alkoxy, or an hydroxy group; R2 and R3 each independently represent a hydrogen or a lower alkyl group; X represents a hydrogen, a lower alkyl, an alkali metal, or an ammonium group; n is an integer of 0 to 3.
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- Inhibiting osteoclast-mediated bone resorption using substituted phenyl derivatives
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Compounds of the general formula Y is an integer of from 0 to 6 is chosen from:, 0, SO2, -CONH-, -NHCO-, -CH2- or, R1 is, substituted or unsubstituted mono- or polycyclic saturated hetero-cyclic ring system having 1, 2 or 3 heteroatoms where said heteroatoms are independently chosen from N, O and S and said substituents are chosen from the group comprising R2;, R2 is, C1 6 alkyl, aryl C0 6alkyl, hydroxy C0 6alkyl, C1 6 alkoxy C0 6alkyl, carboxy C0 6alkyl, oxo, halogen, CF3, C0 4alkylamino-C0 6alkyl or, C0 4dialkylamino-C0 6alkyl;, R3 is, C1 8 alkyl or cycloalkyl, aryl C0 4alkyl, hydroxy C0 4alkyl, C1 4alkyloxy C0 4alkyl, carboxy C0 4alkyl, halogen, CF3 or, hydrogen;, R4 is, hydrogen, C1 6alkyl, aryl C0 4alkyl or, C1 6alkylcarbonyloxymethyl; and, R5 is, C1 6alkyl, aryl C0 4alkyl or, heterocycly C0 4alkyl, and the pharmaceutically acceptable salts thereof; are used for the manufacture of a medicament for treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
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- Method of inhibiting osteoclast-mediated bone resorption by administration of aminoalkyl-substituted phenyl derivatives
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Compounds of the general formula STR1 and the pharmaceutically acceptable salts thereof wherein n is an integer of from 0 to 6; Y is CH2, O, SO2, --CONH--, --NHCO--, or STR2 R1 and R2 are independently hydrogen, C1-8 alkyl, heterocyclyl C0-4 alkyl, aryl C0-4 alkyl, amino C1-4 alkyl, C1-4 alkylamino C1-4 alkyl, or C3-8 cycloalkyl wherein R1 and R2 may be unsubstituted or substituted with one or more groups chosen from R3, where R3 is hydrogen, C1-6 alkyl, hydroxy C0-4 alkyl, carboxy C0-4 alkyl, C1-4 alkyloxy C0-4 alkyl, heterocyclyl C0-4 alkyl, aryl C0-4 alkyl, halogen, or CF3 ; R4 is C1-6 alkyl, heterocyclyl C0-4 alkyl, or aryl C0-4 alkyl; R5 is hydrogen, C1-6 alkyl, aryl C0-3 alkyl, or C1-6 alkylcarbonyloxymethyl are used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.
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- Amplifier molecules for enhancement of diagnosis and therapy
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Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
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- Nucleotide compositions with linking groups
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The present invention includes nucleotide compositions having linking groups and the use and manner of making the nucleotide compositions. The nucleotide compositions are used to attach nonisotopic label moieties to nucleic acid probes.
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- MONOCYCLIC BETA-LACTAMS AND PROCESS FOR THE PREPARATION THEREOF
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Monocyclic beta-lactam compounds represented by the formula STR1 wherein R 1 is H, NH 2, acylamino, C 1 -C 4 alkyl, etc.; R 2 is e.g. C 1 -C 4 alkyl, hydroxyalkyl, aminoalkyl, carboxy, esterified carboxy, esterified carboxyalkyl, or carboxyalkyl; and R 3 is hydrogen, benzyl, substituted benzyl, pivaloyl, --SO 3 M, or --P(C-O)(OM')2; are obtained by the cyclization of an O-substituted hydroxamate of a beta-substituted alkylcarboxylic acid. For example, alpha-ethylmalic acid monobenzyl ester is reacted with O-benzylhydroxylamine to form the O-benzylhydroxamate of the free carboxy group, and the hydroxamate is cyclized with diethyl diazodicarboxylate and triphenylphosphine to form the beta-lactam of the above formula wherein R 1 is ethyl, R 2 is benzyloxycarbonyl and R 3 is benzyl. The beta-lactam compounds are useful intermediates for preparing beta-lactamase inhibitors and monocyclic beta-lactam antibiotics and, when R 3 is --SO 3 M or -P(C-O)(OM')2 the compounds and salts thereof are antibacterial agents.
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- Pharmaceutical products and lactosyl compounds
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The compounds of the formula I exert a pronounced specific cytoprotective effect; they can be used for the treatment of acute and chronic inflammations and organ ischemias caused by narrowing of vessels. R1 denotes an aliphatic radical having 9 to 19 C atoms in the straight chain, R2 denotes the acyl radical of a saturated or unsaturated fatty acid having 14 to 24 C atoms, and X denotes a --CH2 CH2 --or --CH=CH-- group. The invention relates to pharmaceutical products in which the active ingredient is the said compounds, as well as to those compounds I in which R2 denotes the acyl radical of an unsaturated fatty acid, and to the process for the preparation thereof. STR1
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- Antibodies which catalyze hydrolysis of ester bonds
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An analog-ligand having a conformation that substantially corresponds to the conformation of a hydrolytic transition state of an amide or ester reactant ligand is used to produce receptor molecules of predetermined specificity. The receptor molecules include an antibody combining site that binds to a reactant ligand and thereby stabilizes the tetrahedral carbon atom of the amide or ester hydrolysis transition state of that reactant ligand to catalytically hydrolyze the reactant ligand at a predetermined site.
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- Synthetic routes to ninhydrins. Preparation of ninhydrin, 5-methoxyninhydrin, and 5-(methylthio)ninhydrin
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Two syntheses of 5-methoxyninhydrin (2,2-dihydroxy-5-methoxy-1,3-indanedione) are described. One method employs a novel and efficient two step route, which begins with commercially available 6-methoxy-1-indanone. The application of this strategy for the preparation of a new ninhydrin derivative, 5-(methylthio)ninhydrin, and ninhydrin is also presented.
- Heffner,Joullie
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p. 2231 - 2256
(2007/10/02)
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- A Facile One-Pot Synthesis of Vicinal Di- and Triketones from α-Methylene Ketones by NBS-DMSO Oxidation
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The reaction of 1,2-diarylethanones (1a-u) with N-bromosuccinimide in anhydrous dimethyl sulphoxide afforded diarylethanediones (2a-u) in excellent yields.Under similar conditions, 1-phenyl-2-butanone (3) gave 1-phenyl-1,2-butanedione (4) in fair yield in addition to a small amount of 1-phenyl-3-methylthio-1,2-butanedione (5) and 1-phenyl-1-methylthio-2-butanone (6). 4-Phenyl-2-butanone (7), 1,3-diphenyl-2-propanone (9), and 1,3-diphenyl-1,3-propanedione (10) gave the corresponding triketones monohydrate (8) and (11). 1-Indanone (12), 2-indanone (13), and 1,3-indandione (14) gave ninhydrin (15) in good yields.In the case of 3-phenyl-1-indanone (16), 3-phenyl-2-bromo-1-indanone (17), 3-phenyl-2-bromo-1-indenone (18) and 3-phenyl-1-indenone (19) were obtained. 1-Phenyl-1-propanone (20) and 1-phenyl-1-butanone (22) gave the corresponding α-(methylthio)ketones (21) and (22). 1,3,3-Triphenylpropanone (24a) and 1-phenyl-3-methyl-1-butanone (24b) yielded only the corresponding α-bromoketones (25a,b) in good yields.These α-bromoketones, however, afforded the corresponding α-diketones (26a,b) in moderate yields when α-bromoketones reacted with dimethyl sulphoxide in the presence of AgBF4.
- Tatsugi, Jiro,Izawa, Yasuji
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p. 2747 - 2763
(2007/10/02)
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- Singel-Oxygen Photolysis of Dihaloketones. A Facile and Efficient Approach to Vicinal Triketones and Their Monohydrates
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The preparation of vic-triketones and/or their monohydrates by sensitized photooxidation (singlet oxygen) of gem-dihaloketones and/or vic-dihaloketones is described; some reaction mechanisms are discussed.
- Mahran, M. Refat,Abdou, Wafaa M.,Sidky, Mahmoud M.,Wamhoff, Heinrich
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p. 506 - 508
(2007/10/02)
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- N-benzyl,3-hydroxymethyl and 3-alkanoyloxymethyl azetidine derivatives
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Substituted azetidine derivatives of formula STR1 in which R represents chlorine, bromine, hydroxy or alkanoyloxy of up to 6 carbon atoms, processes for their preparation and their use as intermediates for the preparation of azetidine-3-carboxylic acid.
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- Oligopeptide aldehydes useful as specific inhibitors of enterokinase
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Compounds of the general formula: STR1 wherein n is an integer from 2 to 6, m is an integer from 2 to 4, p is an integer from 1 to 3, R is H, an amino protecting group conventionally used in peptide chemistry or a solid phase support, R1 is H or a carboxy protecting group conventionally used in peptide chemistry and R2 is H or alkyl or H2 N--C=NH are useful for inhibiting the activity of enterokinases.
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