138624-99-4Relevant articles and documents
Fungicidal Pyridine Derivatives, IV. α-Trifluoromethyl-3-pyridinemethanols
Sauter, Fritz,Stanetty, Peter,Ramer, Wolfgang,Sittenthaler, Wilhelm
, p. 879 - 885 (1991)
The synthesis of a series of the title compounds is described applying the addition of 3-pyridyllithium to appropriate trifluoromethylalkanones (path 1) and addition of lithiumorganyls to 2,2,2-trifluoro-1-(3-pyridyl)-ethanone (path 2), respectively.Keywords.Fungicides; α-Trifluoromethyl-pyridinemethanols.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0351, (2021/07/31)
Provided herein are novel heterocyclic compounds, for example, compounds having Formula I, I-P, II, lI-P, or III. Also provided herein are pharmaceutical compositions comprising the compounds and methods of using the same, for example, in inhibiting aldehyde dehydrogenases and/or for treating various cancers, cancer metastasis, type 2 diabetes, pulmonary arterial hypertension (PAH) or neointimal hyperplasia (NIH).
One-Pot Successive Turbo Grignard Reactions for the Facile Synthesis of α-Aryl-α-Trifluoromethyl Alcohols
Kani, Ryunosuke,Inuzuka, Toshiyasu,Kubota, Yasuhiro,Funabiki, Kazumasa
supporting information, p. 4487 - 4493 (2020/06/01)
A novel straightforward one-pot methodology for two successive turbo Grignard reagent (iPrMgCl·LiCl) reactions, was developed for a facile synthesis of α-aryl-α-trifluoromethyl alcohols, motifs of value in pharmaceutical chemistry. The method displayed broad functional group tolerance, including reducible groups. Dual roles of iPrMgCl·LiCl were exploited in the tandem reaction with commercially available iodoarenes or iodoheteroarenes and 2,2,2-trifluoroethyl trifluoroacetate. The process encompasses three successive reactions in a one-pot process: the iPrMgCl·LiCl-mediated iodine/magnesium-exchange reaction of iodoarenes or iodoheteroarenes; nucleophilic addition of various generated aryl or heteroarylmagnesium reagents to 2,2,2-trifluoroethyl trifluoroacetate; and the reduction of in-situ generated aryl trifluoromethyl ketones with iPrMgCl·LiCl, to produce the corresponding α-aryl or α-heteroaryl-α-trifluoromethyl alcohols bearing various substituents, including reducible functional groups in good to excellent yields.
FLUOROALKYLATING AGENT
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Paragraph 1343-1344, (2018/01/11)
Problem to be Solved It is intended to provide an industrially preferable fluoroalkylating agent and use thereof. Solution The present invention provides a fluoroalkylating agent represented by the general formula (1) wherein R1 is a C1 to C8 fluoroalkyl group; R2 and R3 are each independently a C1 to C12 alkyl group or the like; Y1 to Y4 are each independently a hydrogen atom, a halogen atom, or the like; and X? is a monovalent anion. A compound of the general formula (3): R4—S—R1 having an introduced C1 to C8 fluoroalkyl group is easily obtained by reacting a compound of the general formula (2): R4—S—Z wherein R4 is a hydrocarbon group or the like; and Z is a leaving group, with the compound of the general formula (1).
TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 50, (2016/03/22)
Provided are quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1, R 2, L, X 1, X 2, and X 3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
Enzyme-catalyzed kinetic resolution of 2,2,2-trifluoro-1-(heteroaryl)ethanols: Experimental and docking studies
Kucher, Olexandr V.,Kolodiazhnaya, Anastasiya O.,Smolii, Oleg B.,Prisuazhnyk, Dmytro V.,Tolmacheva, Katerina A.,Zaporozhets, Olga A.,Moroz, Yurii S.,Mykhailiuk, Pavel K.,Tolmachev, Andrey A.
supporting information, p. 7692 - 7698 (2015/04/22)
A convenient approach towards enantiopure (R) and (S) isomers of 2,2,2-trifluoro-1-(heteroaryl)ethanols was developed. The enzyme-catalyzed kinetic resolution of the corresponding racemic mixtures was achieved by using a two-step protocol that involved an
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND HAVING INHIBITORY EFFECT ON PRODUCTION OF KYNURENINE
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Paragraph 0271, (2013/03/28)
The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R19, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).
KYNURENINE PRODUCTION INHIBITOR
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Page/Page column 132, (2011/10/12)
Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.
Development of fluorination methods using continuous-flow microreactors
Baumann, Marcus,Baxendale, Ian R.,Martin, Laetitia J.,Ley, Steven V.
experimental part, p. 6611 - 6625 (2011/02/25)
The safe and reliable use of various fluorination methods including nucleophilic fluorination (DAST), trifluoromethylation (Ruppert's reagent) and electrophilic fluorination (Selectfluor) in a continuous-flow microreactor is reported. Special a
Trifluoromethylation of carbonyl compounds with trifluoromethyltrimethylsilane (Ruppert reagent) promoted by triphenyldifluorostannates
Borkin,Loska,Makosza
, p. 1187 - 1191 (2007/10/03)
Nucleophilic trifluoromethylation of aromatic aldehydes and ketones with trifluoromethyltrimethylsilane is initiated with KF/n-Bu3MeN +HSO4-/Ph3SnF cocatalytic system in CH2Cl2 or with K[Ph3SnF2] in DMF.