37622-90-5Relevant articles and documents
NAPHTHO[2,1 -D]THIAZOLE DERIVATIVES, COMPOSITIONS THEREOF AND METHODS OF TREATING DISORDERS
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Paragraph 0134, (2021/05/29)
The present application relates to the compounds of formula (I) that inhibit CDK9, pharmaceutical compositions thereof and methods of making and using the same.
Unveiling Potent Photooxidation Behavior of Catalytic Photoreductants
Targos, Karina,Williams, Oliver P.,Wickens, Zachary K.
supporting information, p. 4125 - 4132 (2021/04/07)
We describe a photocatalytic system that reveals latent photooxidant behavior from one of the most reducing conventional photoredox catalysts, N-phenylphenothiazine (PTH). This aerobic photochemical reaction engages difficult to oxidize feedstocks, such as benzene, in C(sp2)-N coupling reactions through direct oxidation. Mechanistic studies are consistent with activation of PTH via photooxidation and with Lewis acid cocatalysts scavenging inhibitors inextricably formed in this process.
Synthesis and preparation method of 4-pyrazole ethyl formate
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Paragraph 0037; 0040-0043; 0046-0049; 0052-0054, (2021/03/13)
The invention discloses a synthesis and preparation method of 4-pyrazole ethyl formate. The method comprises the following steps: dissolving ethyl 2-dichloroacetyl-3-(dimethylamino) acrylate in an organic solvent, and reacting with methylhydrazine to obtain ethyl 1-methyl-3-dichloromethyl-4-pyrazole formate; reacting the obtained ethyl 1-methyl-3-dichloromethyl-4-pyrazole formate with a fluorination reagent to obtain 1-methyl- 3-difluoromethyl-4-pyrazole ethyl formate; mixing 1-methyl- 3-difluoromethyl-4-pyrazole ethyl formate with glacial acetic acid, dropwise adding a strong acidic solutionat the temperature of 0 DEG C, and then adding dichloromethane and water for stirring and layering to obtain an organic layer; and recrystallizing the organic layer by using a mixed solvent of petroleum ether and ethyl acetate to obtain the 4-pyrazole ethyl formate. The method has the advantages of wide raw material source, low raw material price and simple preparation process, and the obtained product is easy to purify, low in production cost and suitable for large-scale industrial production.
Synthetic method of pesticide intermediate pyrazole-4-ethyl formate
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Paragraph 0009, (2017/06/02)
The invention discloses a synthetic method of pesticide intermediate pyrazole-4-ethyl formate. The method comprises the following steps: 1) ethyl cyanoacetate and triethyl orthoformate are placed in a flask, acetic anhydride is added for a reaction, an oil pump is used for performing underpressure distillation to obtain efhylene efhoxymethylene cyanoncetata; 2) efhylene efhoxymethylene cyanoncetata is dissolved in ethanol, hydrazine hydrate is added drop by drop, a solvent is used for underpressure distillation to obtain 3-amino-pyrazoles-4-ethyl formate; and 3) adding pyrazoles-4-ethyl formate and glacial acetic acid are added in a reaction bottle, hydrochloric acid is added drop by drop, a sodium nitrite solution is added drop by drop, after the reaction, ethanol is added for backflow and vacuum concentration, dichloromethane and water are added for stirring and layering, and an organic layer is re-crystallized to obtain the finished product. By employing ester condensation, cyclization and deamination reactions, the preparation technology is simple, and the product is easily purified, production cost is low, and the method is suitable for large-scale industrial production.
Silica supported palladium-phosphine as a reusable catalyst for alkoxycarbonylation and aminocarbonylation of aryl and heteroaryl iodides
Mane, Rajendra Shivaji,Sasaki, Takehiko,Bhanage, Bhalchandra Mahadeo
, p. 94776 - 94785 (2015/11/24)
Silica-supported palladium phosphine complexes were prepared for alkoxycarbonylation and aminocarbonylation of aryl iodides. These catalysts were highly efficient for the carbonylation of unprotected hydroxy-aryl, amino-aryl, iodoindole and iodopyrazole. The carbonylation of unprotected iodopyrazole is challenging and their carbonylation was achieved for the first and obtained corresponding carbonylative products are biologically active. The applicability of developed protocols tolerates wide range of functional groups with excellent yields. The catalyst was easily recovered and shows significant recyclability up to five consecutive cycles without loss in its catalytic activity and selectivity. The prepared catalysts were characterized by different techniques such as FEG-SEM, EDS, FT-IR, XPS and ICP-AES spectroscopy.
Optimization of sphingosine-1-phosphate-1 receptor agonists: Effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles
Skidmore, John,Heer, Jag,Johnson, Christopher N.,Norton, David,Redshaw, Sally,Sweeting, Jennifer,Hurst, David,Cridland, Andrew,Vesey, David,Wall, Ian,Ahmed, Mahmood,Rivers, Dean,Myatt, James,Giblin, Gerard,Philpott, Karen,Kumar, Umesh,Stevens, Alexander,Bit, Rino A.,Haynes, Andrea,Taylor, Simon,Watson, Robert,Witherington, Jason,Demont, Emmanuel,Heightman, Tom D.
supporting information, p. 10424 - 10442 (2015/02/19)
The efficacy of the recently approved drug fingolimod (FTY720) in multiple sclerosis patients results from the action of its phosphate metabolite on sphingosine-1-phosphate S1P1 receptors, while a variety of side effects have been ascribed to its S1P3 receptor activity. Although S1P and phospho-fingolimod share the same structural elements of a zwitterionic headgroup and lipophilic tail, a variety of chemotypes have been found to show S1P1 receptor agonism. Here we describe a study of the tolerance of the S1P1 and S1P3 receptors toward bicyclic heterocycles of systematically varied shape and connectivity incorporating acidic, basic, or zwitterionic headgroups. We compare their physicochemical properties, their performance in in vitro and in vivo pharmacokinetic models, and their efficacy in peripheral lymphocyte lowering. The campaign resulted in the identification of several potent S1P1 receptor agonists with good selectivity vs S1P3 receptors, efficacy at 1 mg/kg oral doses, and developability properties suitable for progression into preclinical development.
Synthesis of 3-substituted-1-methyl-1H-thieno[2,3-c]pyrazoles
Toto, Patrick,Chenault, Jacques,Hakmaoui, Ahmed El,Akssira, Mohamed,Guillaumet, Gerald
, p. 674 - 683 (2008/09/16)
We report a simple and practical six-step synthesis of new 1-methyl-1H-thieno[2,3-c]pyrazoles from 3-amino-1H-pyrazole-4-carboxylic acid ethyl ester. Copyright Taylor & Francis Group, LLC.
Bu3SnH-mediated radical cyclisation onto azoles
Allin, Steven M.,Barton, William R.S.,Russell Bowman,Bridge (née Mann), Emma,Elsegood, Mark R.J.,McInally, Tom,McKee, Vickie
, p. 7745 - 7758 (2008/12/21)
Alkyl radicals have been cyclised onto pyrroles, imidazoles and pyrazoles, and acyl radicals cyclised onto pyrroles, using Bu3SnH-, (TMS)3SiH- and Bu3GeH-mediated aromatic homolytic substitution for the synthesis of bicyclic N-heterocycles. The reactions yield intermediate π-radicals that lose hydrogen in the?rearomatisation step of the aromatic homolytic substitution. Mechanistic studies of these rearomatisation steps indicate aromatic homolytic substitution in which the initiator or breakdown products from the inhibitor are responsible for the H-abstraction step.
Herbicide compositions
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Page/Page column 32, (2010/02/14)
A herbicidal composition which comprises i) an isoxazoline derivative represented by the following general formula (I) or its salt and ii) at least one compound selected from the Group A: Formula (I) wherein R1, R2, R3, R4, R5 and R6 are defined in the specification.
ISOXAZOLINE DERIVATIVE AND HERBICIDE COMPRISING THE SAME AS ACTIVE INGREDIENT
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Page/Page column 196, (2010/02/07)
An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; ???R3, R4, R5 and R6 are each a hydrogen atom; ???Y is an optionally substituted 5- to 6-membered aromatic heterocyclic group or fused aromatic heterocyclic group having a hetero atom selected from a nitrogen atom, a oxygen atom and a sulfur atom; and ???n is an integer of 0 to 2. The isoxazoline derivative has an excellent herbicidal effect and an excellent selectivity between crop and weed.
