76953-96-3Relevant academic research and scientific papers
Fluorine-18 labelled Ruppert-Prakash reagent ([18F]Me3SiCF3) for the synthesis of 18F-trifluoromethylated compounds
Pees, Anna,Vosjan, Maria J.W.D,Vasdev, Neil,Windhorst, Albert D.,Vugts, Danielle J.
supporting information, p. 5286 - 5289 (2021/06/06)
This article describes the first synthesis and application of fluorine-18 labelled Ruppert-Prakash reagent [18F]Me3SiCF3. [18F]Me3SiCF3 was synthesized from [18F]fluoroform with radiochemical yields of 85-95% and radiochemical purities of >95% within 20 m
Construction of trifluoromethylated quaternary stereocenters: Via p -quinone methides
Terashima, Kyu,Kawasaki-Takasuka, Tomoko,Agou, Tomohiro,Kubota, Toshio,Yamazaki, Takashi
, p. 3031 - 3034 (2020/03/19)
Development of a new synthetic method for the construction of quaternary centers with a trifluoromethyl group was realized by way of 1,6-addition of various nucleophiles including active methylene compounds to highly reactive δ-trifluoromethylated p-quinone methides generated in situ from the corresponding tertiary carbonates with a catalytic amount of an appropriate base.
PREPARATION PROCESS OF PERFLUOROALKYL COMPOUND WITH MONOHYDROPERFLUOROALKANE AS STARTING MATERIAL
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Paragraph 0072-0076; 0116; 0117, (2019/06/17)
A simple production process is provided of a perfluoroalkyl compound that uses monohydroperfluoroalkane as a starting material, the perfluoroalkyl compound being an important intermediate of organic electronic materials, medicine, agricultural chemicals,
Organocatalysis approach to trifluoromethylation with fluoroform
Zhang, Yuan,Fujiu, Motohiro,Serizawa, Hiroki,Mikami, Koichi
supporting information, p. 367 - 371 (2014/01/06)
The organic base methodology exploits an access to generate the "trifluoromethyl anion" for carbonyl, ester, acid halide, epoxide, deuterium donor, and carbon dioxide substrates to afford the trifluoromethylation products with good overall efficiency even in organocatalysis conditions. The NMR analysis of the mixture of fluoroform and P4-base shows no change thereof. However, on addition of electrophiles, the trifluoromethylation products were obtained efficiently.
Trifluoromethylation of ketones and aldehydes with Bu3SnCF 3
Sanhueza, Italo A.,Bonney, Karl J.,Nielsen, Mads C.,Schoenebeck, Franziska
, p. 7749 - 7753 (2013/09/02)
The (trifluoromethyl)stannane reagent, Bu3SnCF3, was found to react under CsF activation with ketones and aldehydes to the corresponding trifluoromethylated stannane ether intermediates at room temperature in high yield. Only a mildly acidic extraction (aqueous NH 4Cl) is required to release the corresponding trifluoromethyl alcohol products. The protocol is compatible with acid-sensitive functional groups.
Efficient synthesis of [18F]trifluoromethane and its application in the synthesis of PET tracers
Van Der Born, Dion,Herscheid,Orru, Romano V.A.,Vugts, Danielle J.
, p. 4018 - 4020 (2013/07/26)
A new strategy towards [18F]trifluoromethyl-containing compounds is developed. [18F]trifluoromethane is synthesised in a fast and efficient manner and subsequently used in the reaction with aldehydes and ketones forming [18/sup
4-AMINO-5-OXO-7, 8-DIHYDROPYRIMIDO [5,4-F] [1,4] OXAZEPIN-6 (5H) -YL) PHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Page/Page column 49, (2010/08/09)
The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.
4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
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Page/Page column 37, (2010/08/08)
The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.
BTK protein kinase inhibitors
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Page/Page column 66, (2009/05/29)
This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.
SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 101, (2009/01/20)
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
