- Cis/trans isomerization of o -phosphino-arenesulfonate palladium methyl complexes
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The cis/trans isomerization of (PO-OMe)PdMe(lut) ([PO-OMe]- = 2-{P(2-OMe-Ph)2}-4-Me-benzenesulfonate) was studied to model the proposed isomerization in chain propagation in ethylene polymerization by (o-phosphino-arenesulfonate)PdR(ethylene) species. Nonequilibrium mixtures of cis-P,C- and trans-P,C-(PO-OMe)PdMe(2,6-lutidine) were generated by the reaction of Na[PO-OMe] and {Pd(μ-Cl)Me(2,6-lutidine)}2 in CD2Cl2 at -25 °C. Kinetic studies revealed lutidine-catalyzed and noncatalyzed isomerization pathways. The lutidine-catalyzed pathway involves five-coordinate (PO-OMe)PdMe(lut)2 intermediates that undergo Berry pseudorotation. Kinetic studies, structure-activity relationships, solvent effects, and density functional theory calculations for the noncatalyzed pathway are most consistent with a mechanism, originally proposed by Nozaki, Morokuma, and co-workers, which proceeds through a five-coordinate transition state with κ3-P,O,O coordination of the [PO]- ligand.
- Zhou, Xiaoyuan,Lau, Ka-Cheong,Petro, Benjamin J.,Jordan, Richard F.
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Read Online
- A 2, 6 - dimethyl -4 - bromo pyridine synthesis method
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The invention relates to the field of organic chemistry, in particular to a 2, 6 - dimethyl - 4 - bromo pyridine synthesis method, comprises the following steps: malonic acid diethyl ester and alkali metal reaction to produce salt, then dropwise 4 - nitro - 2 - methyl - 6 chloro pyridine to a toluene solution of a condensation reaction, after decarboxylation under acidic conditions to the 4 - nitro - 2, 6 - dimethyl pyridine; 4 - nitro - 2, 6 - dimethyl pyridine in under the catalysis of the Pd/C, methanol as the solvent, hydrogen reduction, filtered, the filtrate is concentrated, from 4 - amino - 2, 6 - dimethyl pyridine; 4 - amino - 2, 6 - dimethyl pyridine first with an acid generating salt, cooled to - 15 °C - 3 °C, [...], drops the instillment sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, dried, concentrated, be 2, 6 - dimethyl - 4 - bromo pyridine. The method of the invention is beneficial effect: mild reaction conditions, high yield, and raw materials are easy, and the cost is low, the process route is short, and has industrial prospects.
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Paragraph 0011; 0013; 0015; 0017; 0019; 0021
(2019/05/28)
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- Preparation and purification method of toxic impurity DCAL of clopidol
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The invention relates to a preparation and purification method of toxic impurity DCAL of clopidol and belongs to the technical field of preparation of standard medicine products. The preparation and purification method comprises the following steps: firstly carrying out chlorination reaction, i.e., dissolving a solvent and 2,6-dimethyl-4-aminopyridine; then slowly adding a chlorinating agent to carry out chlorination; after reaction is finished, carrying out neutralization and water washing, concentration and crystallization, filtering or direct neutralization and filtering on reaction liquidto obtain a crude DCAL product; purifying the crude DCAL product, adding a mixed solvent of ethanol and ethyl acetate into the crude DCAL product, stirring for dissolving, dripping petroleum ether toprecipitate solids, filtering, carrying out concentration, cooling and precipitation on filtrate, then filtering, and drying solids to obtain a pure DCAL product. The preparation and purification method has the beneficial effects that the reaction temperature is low, the reaction time is short, the side products in reaction are fewer, and the product is easily purified, so that convenience is brought for preparing impurity reference products of the veterinary-drug clopidol.
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Paragraph 0025
(2018/04/03)
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- NEW ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
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The invention provides certain compounds and salts of Formula I and Formula II:which possess antimicrobial activity. The invention also provides novel synthetic intermediatesuseful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8, and Rg are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
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Page/Page column 59; 60
(2008/06/13)
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- 1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO
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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 166-167
(2010/02/11)
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- PYRIDINE DERIVATIVES AND USE THEREOF AS UROTENSIN II ANTAGONISTS
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The invention relates to novel pyridine derivatives of formula 1 and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as neurohormonal antagonists, especially as urotensin II inhibitors.
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Page/Page column 51
(2008/06/13)
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- ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
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The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
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Page/Page column 62-63
(2010/02/11)
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- 1-PYRIDIN-4-YL-UREA DERIVATIVES
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The invention relates to novel 1-pyridyn-4-yl urea derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.
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- Syntheses of five potential heterocyclic amine food mutagens
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The syntheses of the potential heterocyclic amine food mutagens, 3,5,7- trimethyl-2-aminoimidazo[4,5-b]pyridine, 1,4,7-trimethyl-2-aminoimidazo[4,5- c]pyridine, 1,6,7-trimethyl-2-aminoimidazo[4,5-c]-pyridine, 3,4,6-trimethyl- 2-aminoimidazo[4,5-c]pyridine, and 1,4,6-trimethyl-7-aminoimidazo[4,5-c]- pyridine are described.
- Tanga,Bupp,Tochimoto
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p. 717 - 727
(2007/10/03)
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