Category: 386704-04-7

On June 14, 2019, Desi Reddy, Srinivas Reddy; Peri, Seetharamasarma; Rane, Dnyandev Ragho; Donta, Suresh published a patent.Related Products of 386704-04-7 The title of the patent was A process for the preparation 6-trifluoromethylnicotinaldehyde. And the patent contained the following:

The present application provides a process for preparation of 6-trifluoromethylnicotinaldehyde, which is useful as an intermediate for the preparation of Pexidartinib. This process comprises: (a) reacting 5-bromo-2-(trifluoromethyl)pyridine with RMgX [R = Et, Me, Pr and butyl; and X = Cl, F, Br and I] in presence of organic solvent and further treated with paraformaldehyde to produce (6-(trifluoromethyl)pyridin-3-yl)methanol; and (b) oxidizing the latter with MnO2 in presence of organic solvent to produce 6-trifluoromethylnicotinaldehyde. A process for the preparation of 6-trifluoromethylnicotinaldehyde which comprises: (a) reacting 5-bromo-2-(trifluoromethyl)pyridine with RMgX [R and X are as defined above] in presence of organic solvent to produce in-situ of formula I; and (b) reacting I with formylating agent to produce 6-trifluoromethylnicotinaldehyde, is also provided. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Related Products of 386704-04-7

The Article related to trifluoromethylnicotinaldehyde preparation intermediate pexidartinib, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 386704-04-7

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On July 21, 2017, Huang, Qi; Zard, Samir Z. published an article.Computed Properties of 386704-04-7 The title of the article was Modular route to azaindanes. And the article contained the following:

A convergent radical based route to azaindanes, e.g., I, is described, relying on the degenerative addition transfer of various substituted S-(pyridylmethyl)-O-Et dithiocarbonates (xanthates) to functional alkenes followed by radical cyclization onto the pyridine ring activated by protonation with trifluoroacetic acid. In one case, a richly decorated cyclohepta[b]pyridine could be assembled swiftly by allowing the first adduct to N-phenylmaleimide to undergo addition to N-allylphthalimide prior to cyclization. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Computed Properties of 386704-04-7

The Article related to xanthate ester radical cyclization, azaindane preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Computed Properties of 386704-04-7

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On September 20, 2007, Imogai, Hassan Julien; Cid-Nunez, Jose Maria; Andres-Gil, Jose Ignacio; Trabanco-Suarez, Andres Avelino; Oyarzabal Santamarina, Julen; Dautzenberg, Frank Matthias; MacDonald, Gregor James; Pullan, Shirley Elizabeth; Luetjens, Robert Johannes; Duvey, Guillaume Albert Jacques; Nhem, Vanthea; Finn, Terry Patrick; Melikyan, Gagik published a patent.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was 1,4-Disubstituted 3-cyanopyridone derivatives and their use as positive allosteric modulators of mGlu2-receptors and their preparation. And the patent contained the following:

The invention relates to compounds, in particular pyridinone derivatives according to formula I wherein all radicals are defined in the application and claims. Compounds of formula I wherein V1 is a covalent bond and bivalent (un)saturated (un)branched C1-6 hydrocarbon radical; M1 is H, C3-7 cycloalkyl, aryl, alkylcarbonyl, alkyloxy, aryloxy, arylcarbonyl, etc.; L is a covalent bond, O, OCH2, OCH2CH2, OCH2CH2O, OCH2CH2OCH2, S, NH and derivatives, etc.; R2 and R3 are independently H, halo and alkyl; A is (un)substituted Ph, (un)substituted piperazinyl, (un)substituted piperidinyl, (un)substituted thienyl, (un)substituted furanyl, etc.; R4 is halo, CN, OH, oxo, formyl, ethanoyl, carboxyl, NO2, etc.; n is 0, 1, 2, and 3; and their pharmaceutically acceptable acid and addition base salts, stereochem. isomeric forms, N-oxides, and quaternary ammonium salts thereof, are claimed. The compounds according to the invention are pos. allosteric modulators of metabotropic receptors – sub-type 2 (“”mGluR2″”) which are useful for the treatment or prevention of neurol. and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their mGlu-2 receptor modulatory activity. From the assay, it was determined that compound II exhibited a pEC50 value of 6.2. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to disubstituted cyanopyridone preparation mglur2 modulator, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On March 3, 2011, Gradl, Stefan; Laird, Ellen; Moreno, David; Ren, Li; Wenglowsky, Steven Mark published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of 1H-pyrazolo[3,4-b]pyridine compounds useful for inhibiting Raf kinase. And the patent contained the following:

Title compounds I [R1 = H, halo, CN, etc.; R2 and R3 independently = H, halo, alkyl or alkoxy; R4 and R5 independently = H, halo or alkyl; R6 = (un)substituted Ph, 5- to 6-membered heteroaryl, 9- to 10-membered bicyclic heterocyclyl or heteroaryl; R7 = H or methyl], and their stereoisomers, tautomers or pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by cyclization of 5-methoxy-1H-pyrazol-3-amine with sodium nitromalonaldehyde monohydrate followed by reduction and acylation with 3-(benzyloxy)benzoic acid. Compounds of the invention were evaluated for their inhibitory activity of human recombinant B-Raf protein and were found to have an IC50 value of < 1 μM. Methods of using such compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders including cancer in mammalian cells, or associated pathol. conditions are disclosed. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to pyrazolopyridine preparation raf kinase inhibitor cancer, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On January 8, 2021, Zhou, Yaming; Ling, Yun; Deng, Mingli; Jia, Yu; Liu, Xiaofeng; Yang, Yongtai published a patent.Computed Properties of 386704-04-7 The title of the patent was Microwave synthesis method of trifluoromethyl picolinaldehyde. And the patent contained the following:

The present invention relates to a microwave synthesis method of trifluoromethyl picolinaldehyde. The preparation method comprises the following steps of reacting in a reaction tank by using a microwave irradiation technol., calculating according to a chem. equivalent ratio, adding 1 equiv of 6-trifluoromethylpicolinaldehyde methanol, adding a solvent to dissolve, adding 0.01-0.1 equiv of a catalyst and 1-1.5 equiv of an oxidant and setting microwave power and temperature to react after the feeding is finished and after the reaction is finished, carrying out rotary evaporation and concentration on the reaction solution to obtain a solid product and finally carrying out separation and purification to obtain the target 6-trifluoromethyl picolinaldehyde. The inventive method has the advantages of short reaction time, mild conditions, few side reactions and high yield, simplifies the production process, reduces the production cost and cycle and is particularly suitable for the large-scale production of the intermediate 6-trifluoromethyl nicotinaldehyde of a colony stimulating factor 1 receptor (CSF-1R) inhibitor. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Computed Properties of 386704-04-7

The Article related to trifluoromethylpyridine methanol oxidation, trifluoromethyl picolinaldehyde preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Computed Properties of 386704-04-7

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Su, Xiangdong; Pradaux-Caggiano, Fabienne; Vicker, Nigel; Thomas, Mark P.; Halem, Heather; Culler, Michael D.; Potter, Barry V. L. published an article in 2011, the title of the article was Adamantyl Ethanone Pyridyl Derivatives: Potent and Selective Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1.Application of 386704-04-7 And the article contains the following content:

Elevated levels of active glucocorticoids have been implicated in the development of several phenotypes of metabolic syndrome, such as type 2 diabetes and obesity. 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the intracellular conversion of inactive cortisone to cortisol. Selective 11β-HSD1 inhibitors have shown beneficial effects in various conditions, including diabetes, dyslipidemia and obesity. A series of adamantyl ethanone pyridyl derivatives has been identified, providing potent and selective inhibitors of human 11β-HSD1. Lead compounds display low nanomolar inhibition against human and mouse 11β-HSD1 and are selective for this isoform, with no activity against 11β-HSD2 and 17β-HSD1. Structure-activity relationship studies reveal that an unsubstituted pyridine tethered to an adamantyl ethanone motif through an ether or sulfoxide linker provides a suitable pharmacophore for activity. The most potent inhibitors have IC50 values around 34-48 nM against human 11β-HSD1, display reasonable metabolic stability in human liver microsomes, and weak inhibition of key human CYP450 enzymes. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to pyridyl adamantyl ethanone derivative preparation hydroxysteroid dehydrogenase inhibitor sar, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 386704-04-7

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On October 4, 2007, Hannam, Joanne Clare; Hartmann, Sascha; Madin, Andrew; Ridgill, Mark Peter published a patent.Application of 386704-04-7 The title of the patent was Preparation of piperidines and related compounds as γ-secretase modulators for treatment of diseases associated with amyloid beta deposition in the brain. And the patent contained the following:

Title compounds [I; p = 0, 1; q = 0-3; V = bond, C atom bound to H, R2, XZ; W = N, C bound to H, R2, XZ; X = bond, C(R1)2, CH2C(R1)2; Y = bond, CH2, CH2CH2; Z = CO2H, tetrazolyl; R1 = H, nonaromatic hydrocarbyl; R1R1 = atoms to form an alicyclic group; R3, R4 = H; when V, W = C, then R3R4 = CH2CH2; R5 = H, alkyl, fluoroalkyl, alkoxy, fluoroalkoxy, alkenyl; R6 = Het-A; A = bond, CH2, 1,4-phenylene; Het = (substituted) heterocyclyl; R7 = hydrocarbyl optionally bearing a CF3 group; with provisos], were prepared Thus, 6-trifluoromethylnicotinaldehyde (preparation given), 2-methyl-1-buten-3-yne, Me [2-[4-(trifluoromethyl)phenyl]piperidin-4-yl]acetate hydrochloride (preparation given), and AuBr3 were microwaved together in H2O to give 64% ester derivative, which was saponified with LiOH in THF/H2O to give 71% title compound (II). In a cell-based γ-secretase assay, I showed IC50 values for inhibition of Aβ(42) production that were at least 2-fold lower than for Aβ(40). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to piperidineacetate preparation gamma secretase modulator, heteroarylmethyl pentenynyl piperidineacetate preparation amyloid beta disease treatment, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 386704-04-7

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On July 17, 2012, Hannam, Joanne Clare; Hartmann, Sascha; Madin, Andrew; Ridgill, Mark Peter published a patent.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Piperidines and related compounds for the treatment of dementia. And the patent contained the following:

Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer’s disease and related conditions. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to piperidineacetate preparation gamma secretase modulator, heteroarylmethyl pentenynyl piperidineacetate preparation amyloid beta disease treatment, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On May 27, 2010, Carruthers, Nicholas I.; Shireman, Brock T.; Tran, Vi T.; Wong, Victoria D.; Jablonowski, Jill A.; Chai, Wenying published a patent.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Azetidine derivatives and related compounds as serotonin receptor modulators and their preparation and use in the treatment of serotonin-mediated diseases. And the patent contained the following:

The azetidines and related compounds of formula I are serotonin modulators useful in the treatment of serotonin-mediated diseases. Compounds of formula I wherein R1 is H, C1-4 alkyl, monocyclic cycloalkyl, Ph and benzyl; A is (CHR2)n; B is (CHR3)m; m is 1, 2, and 3; n is 1 and 2; with proviso that if m is 2, then n is not 1; R2 and R3 are independently H and C1-4 alkyl; R4 is H, F, C1-4 alkyl; or R4 is OH when L is CH2, CF2, CHF, OCH2 and OCHCH3; L is O, CH2, OCH2, OCHCH3, CH2O, CF2, and CHF; Z is O, CO, OCH2, etc.; R5 is (un)substituted Ph, (un)substituted phenoxy, (un)substituted naphthyl, etc.; X is C and N; R6 and R7 are independently H, halo, CF3, thienyl, and CONH2 and derivatives; and pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, and pharmaceutically active metabolites thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their serotonin receptor modulatory activity (data given). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to azetidine related compound preparation serotonin receptor modulator treatment disease, Heterocyclic Compounds (One Hetero Atom): 4-Membered Rings and other aspects.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On August 4, 2022, Bacani, Genesis M.; Chai, Wenying; Chung, De Michael; Goldberg, Steven D.; Hirst, Gavin; Kaushik, Virendar; Mercado-Marin, Eduardo V.; Raymond, Donald; Seierstad, Mark; Smith, Russel C.; Sundberg, Thomas; Tichenor, Mark S.; Venable, Jennifer D.; Wei, Jianmei; Xavier, Ramnik published a patent.Electric Literature of 386704-04-7 The title of the patent was Heteroaromatics as small molecule inhibitors of salt inducible kinases and their preparation. And the patent contained the following:

Small mol. inhibitors of salt inducible kinases (SIKs) are provided. In particular, compounds of formula I, and tautomers, stereoisomers, pharmaceutically acceptable salts and solvates thereof are provided. Also provided are pharmaceutical compositions containing the compounds, methods of preparing the compounds, and methods of using the compounds for inhibiting SIKs, such as SIK1 and SIK2, and methods of treating diseases mediated by SIKs. Compounds of formula I wherein X1, X2 and X3 are independently N and CH; Q1 and Q2 are independently N and CH; Z is O, OCH2, OCH2CH2 and NH and derivatives, and NHCH2 and derivatives; R1 is COR5, Ph, 5- to 6-membered heteroaryl, etc.; R2 is (un)substituted 4- to 7-membered monocyclic heterocyclyl, (un)substituted 6- to 9-membered bicyclic heterocyclyl, (un)substituted C3-6 cycloalkyl, etc.; R3 is H, Me, Et, propynyl, CN, etc.; R5 is (un)substituted cyclopropyl; and stereoisomers, tautomers, pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by O-arylation of (R)-(1-methylpyrrolidin-3-yl)methanol with N-(5-(5-chloro-2-cyanopyridin-4-yl)pyrazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide. The invention compounds were evaluated for their SIK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 0.00226088μM to 0.0591017μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Electric Literature of 386704-04-7

The Article related to heteroaromatic preparation sik inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Electric Literature of 386704-04-7

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