59938-06-6Relevant articles and documents
Regioselective synthesis of 2-acetyl- and 2-alkoxycarbonyl-3- (trifluoromethyl)phenols by [3+3] cyclization of 1,3-bis-silyl enol ethers with 4-ethoxy- and 4-silyloxy-1,1,1-trifluoroalk-3-en-2-ones
Mamat, Constantin,Pundt, Thomas,Schmidt, Andreas,Langer, Peter
, p. 2183 - 2185 (2006)
2-Acetyl- and 2-alkoxycarbonyl-3-(trifluoromethyl)phenols were prepared by [3+3] cyclization of 1,3-bis-silyl enol ethers with 4-ethoxy- and 4-silyloxy-1,1,1-trifluoroalk-3-en-2-ones.
New air-stable uranium(IV) complexes with enhanced volatility
Leduc, Jennifer,Ravithas, Rajitha,Rathgeber, Lisa,Mathur, Sanjay
, p. 7571 - 7574 (2015)
Herein we report the synthesis and characterization of new air-stable uranium(iv) complexes based on three different heteroarylalkenolate ligands namely DMOPFB (1) (1-(4,5-dimethyl-oxazol-2-yl)-3,3,4,4,4-pentafluoro-but-1-en-2-ol) with an elongated fluori
Fluorinated Cerium(IV) Enaminolates: Alternative Precursors for Chemical Vapor Deposition of CeO2 Thin Films
Schl?fer,Graf,Fornalczyk,Mettenb?rger,Mathur
, p. 5422 - 5429 (2016)
High-yield synthesis of four new fluorinated enaminones LH2 (RfC(O)C2H2NH)2C2H4 (Rf = CF3 (2a), C2F5 (2b), C3F7 (2c)) and (F3CC(O)C2H2NH)2C3H6 (2a′) as dianionic ligands is described. The ligands were characterized in solution (via nuclear magnetic resoannce (NMR)) as well as in the solid state (via X-ray diffraction (XRD)). The ligating ability of the enaminones was verified by reacting them with [Ce2(OiPr)8(HOiPr)2], which resulted in monomeric cerium(IV) complexes [CeL2] (3a-c, 3a′) based on tetradentate chelation of the ligands. Cerium enaminolates were comprehensively analyzed by NMR spectroscopy, mass spectrometry, and single-crystal XRD studies to verify their monomeric nature. High stability under ambient conditions and high volatility makes them a potential precursor for the gas-phase synthesis of CeO2. Complexes 3a and 3b were applied as precursors in thermal and plasma-enhanced chemical vapor deposition to obtain crystalline ceria films with different surface morphologies. The purity and surface states of the films were analyzed by X-ray photoelectron spectroscopy, which revealed a high amount of Ce3+ on the subsurface of CeO2 films.
Continuous preparation method of trifluoromethyl butenone derivative
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Paragraph 0035-0036, (2021/06/22)
The invention discloses a continuous preparation method of a trifluoromethyl butenone derivative. The continuous preparation method is characterized in that a raw material 1 as shown in a structure (I) in a reaction formula and trifluoroacetyl halide serving as a raw material 2 react in a microchannel reactor to prepare the trifluoromethyl butenone derivative as shown in a structure (II). The structure (I) and the structure (II) are as described in the specification. In the structure (I) and the structure (II), R is an electron donating group and can be conjugated with olefin double bonds; R1 and R2 are independently selected from hydrogen, C1-C20 alkyl groups, aryl groups, and substituted aryl groups or silyl groups; and X is halogen and is selected from fluorine, chlorine, bromine and iodine. The method has the advantages of good process universality, good atom economy, high yield, few byproducts, high product purity and the like.
Preparation process 4 - trifluoromethyl nicotinic acid
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Paragraph 0021-0022; 0027-0028; 0033-0034; 0039-0040, (2021/10/11)
The invention discloses a preparation process of 4 -trifluoromethyl nicotinic acid and vinyl ether. Trifluoracetyl chloride and catalyst were added to the reactor and stirred. Acylation to obtain 4 - ethoxy -1, 1, 1 -trifluoro -3 - alkene -2 - ketone, reacting 4 - with a catalyst and an oxidizing agent to -1 ethoxy 1, 1 -3 -trifluoro -2 -butenone, 25 - 90 °C g 30 - 60min of 1-trifluoroethyl 1-butenecone, adding 1 - equivalents of alkali lye, and then acidifying to obtain -4 - 2-trifluoromethylnicotiniconicotinic acid, followed by acidification with -3 - 4 -chloro 1 - 5-4 - trifluoromethyl POCl3 picolinic 6 - acid -4 . The preparation method of 4 -trifluoromethyl nicotinic acid is optimized. Only the reaction temperature is controlled, the intermediate product can be used for subsequent reaction steps, the reaction requirements in the step process are reduced, the requirement for equipment is low, and industrialization can be conveniently realized.
KRAS G12C Mutant protein inhibitor and pharmaceutical composition thereof Preparation method and application
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Paragraph 0191; 0193; 0197-0199, (2021/10/27)
The present invention provides compounds having irreversible inhibitor activity G12C mutant KRAS protein, racemates, stereoisomers, pharmaceutically acceptable salts, polymorphs or solvates thereof, the structure of which is shown in formula (I). Also provided are methods related to the preparation and use of such compounds, pharmaceutical compositions comprising such compounds, and methods of modulating G12C mutant KRAS protein activity for treatment of disorders such as cancer.
2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists
Ann, Jihyae,Bahrenberg, Gregor,Blumberg, Peter M.,Choi, Sun,Christoph, Thomas,Do, Nayeon,Frank-Foltyn, Robert,Ha, Heejin,Jeong, Jin Ju,Kang, Jin Mi,Kim, Changhoon,Kwon, Sun Ok,Lee, Jeewoo,Lee, Sunho,Lesch, Bernhard,Stockhausen, Hannelore,Vu, Thi Ngoc Lan,Yoon, Sanghee
, (2021/07/28)
A series consisting of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists. The structure–activity analysis targeting their three pharmacophoric regions indicated that halogenated phenyl A-region analogs exhibited a broad functional profile ranging from agonism to antagonism. Among the compounds, antagonists 28 and 92 exhibited potent antagonism toward capsaicin for hTRPV1 with Ki[CAP] = 2.6 and 6.9 nM, respectively. Further, antagonist 92 displayed promising analgesic activity in vivo in both phases of the formalin mouse pain model. A molecular modeling study of 92 indicated that the two fluoro groups in the A-region made hydrophobic interactions with the receptor.
Preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine
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Paragraph 0017; 0020; 0023; 0026; 0029; 0032; 0035; 0038, (2021/07/17)
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine, and the preparation method of N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine comprises the following steps: taking trifluoroacetic acid, vinyl ethyl ether, methylsulfonyl chloride and pyridine as raw materials, firstly preparing 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-ketone, carrying out ammonia ammoniation to obtain 4-amino-1, 1, 1-trifluoro-3-butene-2-ketone, then, under the action of sodium hydroxide, reacting with methyl 3-methoxyacrylate to obtain a target product N-(2-methoxycarbonyl vinyl)-4, 4, 4-trifluoro-3-ketone-1-buteneamine. The adopted raw materials are relatively cheap and easy to obtain, and the method is easy and convenient to operate, safe, feasible, high in cost performance and suitable for industrial production.
Continuous synthesis method of 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-one
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Paragraph 0040-0077, (2020/05/08)
The invention provides a continuous synthesis method of 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-one. The continuous synthesis method comprises the following steps: enabling raw materials containing vinyl ethyl ether, triethylamine and trifluoroacetic anhydride to continuously enter a continuous reactor to react so as to obtain a product system containing the 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-one; performing continuous extraction on the product system to obtain the 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-one, and performing continuous extraction on the product system to obtain the 4-ethoxy-1, 1, 1-trifluoro-3-butene-2-one. By using a continuous process, the raw materials can be conveniently and accurately pumped into the continuous reactor, and after the reaction is finished, continuous extraction is also used for post-treatment, so that the whole process is quick, simple and efficient, the efficiency of the whole synthesis process is greatly improved, and the damage loss of a product is reduced; and the potential safety hazard of batch production is avoided. After amplification, an amplification effect does not exist, and safety and high synthesis efficiency can still be kept.
Nanostructured IrOx Coatings for Efficient Oxygen Evolution Reactions in PV-EC Setup
Jürgensen, Lasse,Frank, Michael,Graf, David,Gessner, Isabel,Fischer, Thomas,Welter, Katharina,J?germann, Wolfram,Mathur, Sanjay
, p. 911 - 924 (2020/03/19)
New heteroleptic iridium compounds exhibiting high volatility and defined thermal decomposition behavior were developed and tested in plasma-enhanced chemical vapor deposition (PECVD). The iridium precursor [(COD)Ir(TFB-TFEA)] (COD = 1,5-cyclooctadiene; TFB-TFEA = N-(4,4,4-Trifluorobut-1-en-3-on)-6,6,6-trifluoroethylamin) unifies both reactivity and sufficient stability through its heteroleptic constitution to offer a step-by-step elimination of ligands to provide high compositional purity in CVD deposits. The substitution of neutral COD ligands against CO groups further increased the volatility of the precursor. PECVD experiments with unambiguously characterized Ir compounds (single crystal X-ray diffraction analysis) demonstrated their suitability for an atom-efficient (high molecule-to-precursor yield) gas phase deposition of amorphous iridium oxide (IrOx) phases. Thin films of IrOx were well suited as electrocatalyst in oxygen evolution reaction so that an efficient coupled system in combination with solar cells is viable to perform water-splitting reaction without external bias.
