Category: 386704-04-7

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Zhu, Lei published a patent.Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted (azabicycloalkyl)indoles and (azabicycloalkyl)pyridoindoles as MCH-1 receptor antagonists and use in the treatment of diseases. And the patent contained the following:

Title compounds I [R1 = H, (un)substituted alkyl, cycloalkyl, heteroaryl, etc; each R2 independently = H, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; R3 = H, halo, (un)substituted aryl, heteroaryl, etc.; A = (CH2)n; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR9, C(R9)2, N, or NR9; Y = CR9, C, or N; Z = CH, C, or N; R9 = H, halo, NH2 and derivatives, (un)substituted alkyl etc.; m = 0 to 3, n = 1 or 2; p = 1 to 4; dash bond represents an optional double bound], and their pharmaceutically acceptable salts, oxides, solvates, or prodrugs, are prepared and disclosed as MCH-1 receptor antagonists and useful in the treatment of obesity, anxiety, depression, non-alc. fatty liver disease, and psychiatric disorders. Thus, e.g., II·HCl was prepared by methylation of 3-bromophenylhydrazine hydrochloride with Me iodide followed by heterocyclization with 1-azabicyclo[3,2,1]octan-4-one, amination with 4-(benzyloxy)pyridin-2(1H)-one, and addition of hydrochloric acid. Select I were evaluated for their MCH-1 antagonistic activity, e.g., II·HCl demonstrated a Ki value of 6.4 nM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to azinone azabicycloalkyl indole preparation mch1 receptor antagonist treatment disease, azabicycloalkyl pyridoindole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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Alcohol – Wikipedia,
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On March 10, 2021, Lesch, Bernhard; Jakob, Florian; Pletinckx, Katrien; Arndt, Verena; Wagener, Markus; Dunkern, Torsten published a patent.Electric Literature of 386704-04-7 The title of the patent was Preparation of piperidines or piperidones substituted with urea and heteroaryl as FPR2 modulators. And the patent contained the following:

The invention relates to compounds of formula I which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2 which include but are not limited to inflammatory and autoimmune diseases, diabetes, obstructive airway disorders, sepsis, etc. Compounds of formula I [wherein X1 = CH2, or C(O) and X2 = CH2; or X2 = CH2 or C(O) and X1 = CH2; R1 = Ph or 5 or 6-membered heteroaryl; Z = 5 or 6-membered heteroaryl which mono-, di, or trisubstituted with R2; each R2 independently = H, F, Cl, CF3, etc.; L = bond, C1-6alkylene, C(O), S(O)2, etc.; R3 = H, C1-6alkyl, C3-6cycloalkyl, 3-to 6-membered heterocycloalkyl, etc.; wherein C1-6alkyl in each case independently from one another is linear or branched, saturated or unsaturated; wherein C1-6alkylene is linear and saturated or unsaturated; wherein C1-6alkyl, C1-6alkylene, C3-6cycloalkyl, and 3 to 6-membered heterocycloalkyl in each case independently from one another are unsubstituted or mono- or polysubstituted; with proviso] in form of free compounds or physiol. acceptable salts thereof, are claimed and exemplified. Example compound II was synthesized from the reaction of prepared intermediate trans-1-(4-chloro-phenyl)-3-(6′-methoxy-1,2,3,4,5,6-hexahydro-3,3′-bipyridinyl-4-yl)-urea hydrochloride with 4-iodo-pyrimidine in the presence of L-proline and CuI in 14% yield. Candidate compounds of formula I were evaluated for agonistic activity using hFPR2-Aq-CHO cells from which II demonstrated an EC50 = 0.00600μM. 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 piperidine urea heteroaryl derivative preparation fpr2 inflammatory autoimmune disease, piperidone urea heteroaryl derivative preparation diabetes obstructive airway disorder and other aspects.Electric Literature of 386704-04-7

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On January 15, 2009, Dalence, Maria; Johansson, Martin; Thornqvist Oltner, Viveca; Toftered, Joergen; Wensbo, David published a patent.Recommanded Product: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of novel bronchodilating isoquinoline carbamates. And the patent contained the following:

The title compounds I [R1, R2 = H or Me; R3, R4 = H, F, Cl, Br, alkyl, benzyl; G = (un)substituted alkylene(hetero)aryl; with the proviso that not both of R1 and R2 is Me; and the exclusion of 3 compounds], useful to manufacture a medicament to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma, and by vasoconstriction, e.g. hypertension, were prepared E.g., a 3-step synthesis of I [R1, R2 = H; R3, R4 = Cl; G = CH2Ph], starting from 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride, was given. Exemplified compounds I were tested for their biol. activity. For example, pre-treatment with I [R1, R2 = H; R3, R4 = Cl; G = CH2Ph] resulted in 38% remaining contraction of human bronchiols after leukotriene D4 (10 nM) induced contraction. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Recommanded Product: (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to isoquinoline carbamate preparation bronchodilator bronchoconstriction vasoconstriction copd asthma hypertension, antiasthmatic antihypertensive isoquinoline carbamate preparation and other aspects.Recommanded Product: (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On June 30, 2016, Sato, Takahiro; Nagayama, Sachiho; Yoshino, Yasuhiro; Inoue, Tsutomu; Kato, Hiroshige; Uda, Junichiro; Inaba, Masato; Yamoto, Noriko; Taniguchi, Tetsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of novel heterocyclic derivative as EPO production promoters for prevention or treatment of anemia. And the patent contained the following:

The present invention relates to a compound represented by the following general formula I [wherein X represents an oxygen atom, an imino group, a sulfur atom, sulfinyl, or sulfonyl, R1, R2, and R3 each independently represent a hydrogen atom or a C1-6 alkyl group, R4 represents a hydrogen atom, a C1-6 alkyl group, or an arylalkyl group, R5 represents an alkyl, alkenyl, alkynyl, aryl, or heteroaryl group]. This compound has excellent EPO-production acceleration activity and is useful as a pharmaceutical. Thus, addition of [5-(3,5-dichlorophenylsulfanyl)-7-hydroxy[1,2,4]triazolo[1,5-a]pyridine-8-carbonylamino]acetic acid, prepared from 3,5-dichlorobenzenethiol and 7-benzyloxy-5-iodo[1,2,4]triazolo[1,5-α]pyridine-8-carboxylic acid tert-Bu ester, to culture of Hep3B cells significantly increased erythropoietin production The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7

The Article related to heterocyclic amide compound preparation erythropoietin production promoter treatment anemia, triazolopyridinecarboxamidoacetic acid erythropoietin production promoter antianemic drug and other aspects.HPLC of Formula: 386704-04-7

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Murugesan, Dinakaran; Kaiser, Marcel; White, Karen L.; Norval, Suzanne; Riley, Jennifer; Wyatt, Paul G.; Charman, Susan A.; Read, Kevin D.; Yeates, Clive; Gilbert, Ian H. published an article in 2013, the title of the article was Structure-Activity Relationship Studies of Pyrrolone Antimalarial Agents.Related Products of 386704-04-7 And the article contains the following content:

Previously reported pyrrolones, such as TDR32570 (I), exhibited potential as antimalarial agents; however, while these compounds have potent antimalarial activity, they suffer from poor aqueous solubility and metabolic instability. Here, further structure-activity relationship studies are described that aimed to solve the developability issues associated with this series of compounds In particular, further modifications to the lead pyrrolone, involving replacement of a Ph ring with a piperidine and removal of a potentially metabolically labile ester by a scaffold hop, gave rise to derivatives with improved in vitro antimalarial activities against Plasmodium falciparum K1, a chloroquine- and pyrimethamine-resistant parasite strain, with some derivatives exhibiting good selectivity for parasite over mammalian (L6) cells. Three representative compounds were selected for evaluation in a rodent model of malaria infection, and the best compound showed improved ability to decrease parasitemia and a slight increase in survival. 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 pyrrolone piperidine containing preparation antimalarial structure activity relationship, plasmodium falciparum, antiprotozoal agents, malaria, pyrrolones, structure-activity relationships and other aspects.Related Products of 386704-04-7

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Alcohol – Wikipedia,
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On September 14, 2017, Bollinger, Katrina A.; Felts, Andrew S.; Brassard, Christopher J.; Engers, Julie L.; Rodriguez, Alice L.; Weiner, Rebecca L.; Cho, Hyekyung P.; Chang, Sichen; Bubser, Michael; Jones, Carrie K.; Blobaum, Anna L.; Niswender, Colleen M.; Conn, P. Jeffrey; Emmitte, Kyle A.; Lindsley, Craig W. published an article.Related Products of 386704-04-7 The title of the article was Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. And the article contained the following:

Herein, the authors detail the optimization of the mGlu2 neg. allosteric modulator (NAM), 4-(4-fluorophenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (VU6001192), by a reductionist approach to afford a novel, simplified mGlu2 NAM scaffold. This new chemotype not only affords potent and selective mGlu2 inhibition, as exemplified by VU6001966 (mGlu2 IC50 = 78 nM, mGlu3 IC50 > 30 μM), but also excellent central nervous system (CNS) penetration (Kp = 1.9, Kp,uu = 0.78), a feature devoid in all previously disclosed mGlu2 NAMs (Kps ≈ 0.3, Kp,uus ≈ 0.1). Moreover, this series, based on overall properties, represents an exciting lead series for potential mGlu2 PET tracer development. 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 mglu2 central nervous system penetration picolinamide pharmacokinetics, cns penetration, negative allosteric modulator (nam), vu6001966, depression, metabotropic glutamate receptor 2 (mglu2) and other aspects.Related Products of 386704-04-7

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Drouet, Fleur; Noisier, Anais F. M.; Harris, Craig S.; Furkert, Daniel P.; Brimble, Margaret A. published an article in 2014, the title of the article was A Convenient Method for the Asymmetric Synthesis of Fluorinated α-Amino Acids from Alcohols.Related Products of 386704-04-7 And the article contains the following content:

Due to their numerous applications, fluorinated amino acids have recently attracted significant attention. The preparation of fluorine-containing phenylalanines and aliphatic fluorinated amino acids using Mitsunobu-Tsunoda alkylation of a chiral nucleophilic glycine equivalent with readily available alc. substrates is described. The reaction proceeds in high yields and with excellent diastereoselectivity. This method provides an efficient synthetic route to fluorinated amino acids for which asym. approaches are scarce. 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 fluorinated amino acid asym preparation, aliphatic fluorinated amino acid asym preparation, phenylalanine fluorinated asym preparation, mitsunobu tsunoda alkylation chiral glycine nickel complex fluorinated alc and other aspects.Related Products of 386704-04-7

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Alcohol – Wikipedia,
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On September 3, 2009, Vicker, Nigel; Su, Xiangdong; Pradaux-Caggiano, Fabienne; Potter, Barry Victor Lloyd published a patent.Category: alcohols-buliding-blocks The title of the patent was Adamantyl, phenyl, and benzyl ketone derivatives as inhibitors of 11β-hydroxysteroid dehydrogenase type I useful in the treatment of diseases and preparation and pharmaceutical compositions thereof. And the patent contained the following:

Title compounds I and their pharmaceutical compositions are prepared and disclosed as inhibitors of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1) useful in the treatment of diseases. Compounds I [X and Z independently = (un)saturated C1-3 carbon chain; Y = S, SO, SO2, CH=CH, CH2CH2, or O; R1 = 1-adamantyl, 2,4,6-trimethylphenyl, 1-(4-chlorophenyl)C3-6 cycloalkyl, or 2-(4-chlorophenyl)propan-2-yl; R2 = (un)substituted 5- to 6- membered N-containing heteroaryl; with the provision that when R1 = 1-adamantyl and X-Y-Z = CH2S, CH2SO, or CH2SO2, then R2 ≠ 1-methylimidazol-2-yl; or when R1 = 1-adamantyl and X-Y-Z = CH2O, then R2 ≠ 2-methylpyridinyl] are claimed. For example, compound II was prepared via substitution of 2-bromo-1-[1-(4-chlorophenyl)cyclopropyl]ethanone with 2-mercapto-1-methylimidazole. Select I were assayed for 11β-HSD1 inhibition and compound II was found to possess >60% inhibition at 1 μM concentration The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Category: alcohols-buliding-blocks

The Article related to adamantyl ketone derivative preparation 11 beta hydroxysteroid dehydrogenase inhibitor, phenyl ketone derivative preparation 11 beta hsd1 inhibitor, benzyl ketone preparation 11 beta hydroxysteroid dehydrogenase type i and other aspects.Category: alcohols-buliding-blocks

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On September 30, 2004, Goble, Stephen D.; Pasternak, Alexander; Mills, Sander G.; Zhou, Changyou; Yang, Lihu published a patent.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of (tetrahydropyranylamino)cyclopentanecarbonyl-substituted fused azaheterocycles as modulators of cytokine receptors such as CCR2. And the patent contained the following:

Compounds I [A = R82C, C(:O), NR8, O; B = R22C, O, S(:O), SO2, NSO2R14, NC(:O)R13, NC(:O)NR122,C(:O); D, X = C, N; E = (CH2)n; G = CH:CH, CH2CH2; Y = O, R12N, S, S(:O), SO2, R112C, etc.; n = 0-2; R1 = H, NC, (un)substituted alkyl, heterocyclyl, Ph, R122N, R13C(:O)N(R12), R14SO2N(R12), R11C(:O), R122NC(:O); R2 = H, alkyl, F, HO, heterocyclyl, R13C(:O)NH, etc.; R3, R4 = absent, H, (un)substituted alkyl, HO, Cl, O, etc.; R5 = (un)substituted alkyl, alkoxy, alkylcarbonyl, alkylthio, pyridyl, etc.; R8 = H, alkyl, (un)substituted alkylcarbonylalkyl; R11 = HO, H, (un)substituted alkyl, alkoxy, cycloalkyl, benzyl, phenyl; R12 = H, (un)substituted alkyl, benzyl, Ph, cycloalkyl; R13 = H, (un)substituted alkyl, alkoxy, benzyl, Ph, cycloalkyl; R14 = H, HO, (un)substituted alkyl, benzyl, Ph, cycloalkyl; R15 = H, (un)substituted alkyl; R16 = H, (un)substituted alkyl, alkoxy, cycloalkyl, F, HO, etc.; R17 = H, HO, (un)substituted alkyl, alkoxy, R11C(:O); R18 = H, F, (un)substituted alkyl, cycloalkoxy, alkoxy; R16 and either R17 or R18 may be joined in a ring] such as II are prepared as modulators of cytokine receptors such as CCR2 for the treatment of inflammatory and immune system disorders such as rheumatoid arthritis. Coupling of (tert-butoxy)(trifluoromethyl)benzylamine III and nonracemic (tetrahydropyranylamino)cyclopentanecarboxylic acid IV followed by cleavage of the tert-Bu group, cyclocondensation with paraformaldehyde, and cleavage of the trifluoroacetamide yields II as its hydrochloride salt. III is prepared by nucleophilic substitution of 2-fluoro-5-(trifluoromethyl)benzonitrile with potassium tert-butoxide followed by hydrogenation of the nitrile moiety. IV is prepared by Boc protection of the amine moiety of V, benzylation of the carboxylic acid group, cleavage of the Boc group, reductive amination of the amine with tetrahydropyran-4-one, trifluoroacetylation of the secondary amine, stereoselective alkylation of the ester with potassium bis(trimethylsilyl)amide and iso-Pr iodide, and hydrogenolysis of the benzyl ester; a second route to IV is also described. Compounds of the invention inhibit CCR2 with IC50 values of < 1 μM (no data). 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 tetrahydropyranylamino cyclopentanecarbonyl substituted fused azaheterocycle preparation cytokine receptor modulator, ccr2 modulator tetrahydropyranylamino cyclopentanecarbonyl substituted fused azaheterocycle preparation and other aspects.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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On September 16, 2010, Ahmad, Saleem published a patent.Synthetic Route of 386704-04-7 The title of the patent was Preparation of aza-pyridone derivatives as antagonists of melanin concentrating hormone receptor-1 (MCHR1). And the patent contained the following:

Title compounds I [A1 and A2 independently = C or N; E = C or N; Q1, Q2 and Q3 independently = C or N provided that only one of them is N; D1 = bond, CC, 1,2-cyclopropyl, etc; R1, R2 and R3 independently = H, halogen, (un)substituted alkyl, etc; G = O, S or NR15; where R15 = H or (un)substituted alkyl; D2 = (un)substituted alkyl, cycloalkyl, cycloalkoxy, etc; Z1 and Z2 independently = H, (un)substituted alkyl, cycloalkyl, etc; R5, R6 and R7 independently = H, halogen, (un)substituted alkyl, etc], and their pharmaceutically acceptable salts or prodrugs, are prepared and disclosed. Thus, e.g., II was prepared by coupling reaction of (E)-4-chlorostyrylboronic acid with 6-chloro-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)pyrimidin-4(3H)-one (preparation given). Compounds of the invention were evaluated for their antagonistic activity of peptide agonist binding to human melanin concentrating hormone receptor-1 (MCHR1), e.g., II exhibited Ki value of 23 nM. The invention compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, inflammatory bowel disease, depression, and anxiety. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Synthetic Route of 386704-04-7

The Article related to aza pyridone preparation melanin concentrating hormone receptor antagonist, obesity diabetes depression anxiety mchr1 antagonist pyrimidinone preparation, inflammatory bowel disease mchr1 antagonist pyridazinone preparation and other aspects.Synthetic Route of 386704-04-7

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