1823-63-8Relevant academic research and scientific papers
Direct Synthesis of Tri-/Difluoromethyl Ketones from Carboxylic Acids by Cross-Coupling with Acyloxyphosphonium Ions
Ispizua-Rodriguez, Xanath,Munoz, Socrates B.,Krishnamurti, Vinayak,Mathew, Thomas,Prakash
supporting information, p. 15908 - 15913 (2021/10/07)
A simple and straightforward approach to the synthesis of trifluoromethyl and difluoromethyl ketones from widely available carboxylic acids is disclosed. The transformation utilizes an acyloxyphosphonium ion as the active electrophile, conveniently generated in situ from the carboxylic acid substrate by using commodity chemicals. The utility of the reaction system is exemplified by its chemoselectivity, with tolerance to a variety of important functional groups. The late-stage functionalization of carboxylic acid active pharmaceutical ingredients and pharmaceutically relevant compounds is also discussed.
Asymmetric synthesis of photophore-containing lactisole derivatives to elucidate sweet taste receptors
Hashimoto, Makoto,Ishida, Akiko,Misaka, Takumi,Nakagita, Tomoya,Tachrim, Zetryana Puteri,Wang, Lei
, (2020/06/30)
Lactisole, which has a 2-phenoxy propionic acid skeleton, is well-known as an inhibitor of sweet taste receptors. We recently revealed some of the structure-activity relationships of the aromatic ring and chiral center of lactisole. Photoaffinity labeling
COMPOUNDS AND METHODS FOR REGULATING INSULIN SECRETION
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Page/Page column 112, (2018/10/19)
Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods.
Mechanogeneration of Acid from Oxime Sulfonates
Nagamani, Chikkannagari,Liu, Huiying,Moore, Jeffrey S.
supporting information, p. 2540 - 2543 (2016/03/12)
The generation of acid under mechanical force is potentially useful for initiating proton-catalyzed changes in polymeric materials. Here we demonstrate that oxime sulfonates - known photoacid generators - are also acid generators when activated mechanical
Stereoselective metal-free catalytic synthesis of chiral trifluoromethyl aryl and alkyl amines
Genoni, Andrea,Benaglia, Maurizio,Massolo, Elisabetta,Rossi, Sergio
supporting information, p. 8365 - 8367 (2013/09/23)
The enantioselective organocatalytic reduction of trifluoromethyl aryl and alkyl ketoimines afforded the corresponding fluorinated amines with high chemical and stereochemical efficiency. The Lewis base catalyzed reaction with trichlorosilane led to chiral products with a trifluoromethyl group directly linked to the newly generated stereocenter typically in >90% yield and up to 98% e.e.
Highly efficient synthesis of aryl and heteroaryl trifluoromethyl ketones via o-iodobenzoic acid (IBX)
Cheng, Huicheng,Pei, Yu,Leng, Faqiang,Li, Jingya,Liang, Apeng,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
, p. 4483 - 4486 (2013/07/26)
A two-step process for the synthesis of aryl and heteroaryl trifluoromethyl ketones from the corresponding aldehydes is described. Trifluoromethyl alcohols were prepared from aryl and heteroaryl aldehydes in excellent yields using catalytic amount of K2CO3. The trifluoromethyl alcohols were then oxidized conveniently and efficiently by o-iodoxybenzoic acid (IBX) under mild conditions to get the desired functionalized aryl and heteroaryl trifluoromethyl ketones.
A generic small-molecule microarray immobilization strategy
Valls-Miret, Mariona,Bradley, Mark
scheme or table, p. 6819 - 6822 (2012/01/02)
Small-molecule microarrays are often limited by the requirement for each compound undergoing immobilization to contain a common functional group or by the need to prepare glass slides containing photo-reactive groups. Herein, we present a generic strategy
BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 168, (2010/11/27)
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 A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
Poly(ethylene glycol)-supported ααα-trifluoroacetophenone in dioxirane mediated alkene epoxidation reactions
Kan, Jovi Tze Wai,Toy, Patrick
, p. 6357 - 6359 (2007/10/03)
Poly(ethylene glycol) (PEG) was used for the immobilization of ααα-trifluoroacetophenone and the utility of this supported ketone has been examined in dioxirane mediated epoxidation of alkenes. The PEG-ketone reagent was found to be an effective homogeneous catalyst for the epoxidation of a variety of alkenes in the presence of Oxone A? and was readily recovered from the reaction mixtures and reused.
Total synthesis of two photoactivatable analogues of the growth-factor-like mediator sphingosine 1-phosphate: Differential interaction with protein targets
Lu, Xuequan,Cseh, Sandor,Byun, Hoe-Sup,Tigyi, Gabor,Bittman, Robert
, p. 7046 - 7050 (2007/10/03)
The first synthesis of two photoreactive analogues of the lipid mediator and second messenger sphingosine 1-phosphate (S1P), [32P]-labeled (2S,3R)-14-O-(4′-benzoylphenyl)- and (2S,3R)-14-O-((4′ -trifluoromethyldiazirinyl)phenyl)-(4E) -tetradece
