Month: November 2022

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Henderson, Alan John; Jiang, May Xiaowu published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted azapolycycles 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, alkenyl, alkynyl, etc; R2 and R4 independently = H, CONH2 and derivatives, (un)substituted alkyl, aryl, etc.; R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; at least one of R2 and R3 or R3 and R4 taken together to form an (un)substituted 3- to 7-membered heterocycle; each R5 independently = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; R6 = H, halo, (un)substituted aryl, heteroaryl, etc.; A = (CH2)m; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; D = (CH2)n; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR12, C(R12)2, N, or NR12; Y = CR12, C, or N; Z = CH, C, or N; R12 = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; m and n = 0 or 1, wherein m + n = 1; p = 1 to 4; q = 0 to 3; 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 acylation of 2-(6-bromo-1-methyl-1H-indol-3-yl)ethanamine with 4-bromobutyryl chloride followed by intramol. cyclization, intramol. reductive N-alkylation, 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 14.9 nM. 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 azinone azapolycycle preparation mch receptor antagonist treatment disease, 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.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On June 21, 2007, Vanotti, Ermes; Menichincheri, Maria; Orsini, Paolo; Scolaro, Alessandra; Varasi, Mario published a patent.Electric Literature of 87674-15-5 The title of the patent was Preparation of N-substituted pyrrolopyridinones active as kinase inhibitors. And the patent contained the following:

The title compounds I [A = pyridin-4-yl, 3-fluoropyridin-4-yl, 2-aminopyrimidin-4-yl; R1 = H, halo, alkyl; R2 = alkyl, cycloalkyl, aryl, etc.; R3-R6 = H, alkyl, aryl, etc.], useful as Cdk2 or Cdc7 antagonists, were prepared Thus, reacting tert-Bu 2-(2-aminopyrimidin-4-yl)-4-oxo-1,4,6,7-tetrahydropyrrolo[3,2-c]pyridine-5-carboxylate with 1-bromo-2-fluoroethane followed by deprotection afforded 2-(2-aminopyrimidin-4-yl)-1-(2-fluoroethyl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Electric Literature of 87674-15-5

The Article related to pyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor antagonist, 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.Electric Literature of 87674-15-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On August 30, 2007, Vanotti, Ermes; Martina, Katia; Menichincheri, Maria; D’Alessio, Roberto published a patent.Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol The title of the patent was Preparation of pyrrolopyrrolones as kinase inhibitors for treating cancer and other diseases. And the patent contained the following:

Compounds represented by formula I (wherein A is pyridin-4-yl, 3-fluoropyridin-4-yl, and 2-aminopyrimidin-4-yl; R1 is H, halo, and (C1-C6)alkyl; R2 is H, (C1-C6)alkyl, (C2-C6)alkenyl, etc.; R3 and R4 are H, (C1-C6)alkyl, (C3-C6)cycloalkyl, etc., or taken together form a (C3-C6)cycloalkyl), compositions thereof, and methods of use thereof. I are useful, in therapy, as agents against a host of diseases caused by and/or associated to a disregulated protein kinase activity and more particularly, Cdk2 and Cdc7 activity. I have protein kinase inhibiting activity and more particularly, Cdk2 and Cdc7 inhibiting activity; no biol. data is given in the patent. Example compound II was synthesized by cyclization of DL-2-(1-Amino-2-benzyloxyethyl)-5-(2-aminopyrimidin-4-yl)-1H-pyrrole-3-carboxylic acid. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol

The Article related to pyrrolopyrrolone preparation kinase inhibitor cancer other disease treatment, 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.Quality Control of 1-(3-Fluoropyridin-4-yl)ethanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 31, 2016, Cai, Jiaqiang; Colandrea, Vincent; Crespo, Alejandro; Debenham, John; Du, Xiaoxing; Guiadeen, Deodialsingh; Liu, Ping; Liu, Rongqiang; Madsen-Duggan, Cristina B.; McCoy, Joshua G.; Quan, Weiguo; Sinz, Christopher; Wang, Liping published a patent.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Quinolinecarboxamidoacetic acids and related compounds as inhibitors of HIF prolyl hydroxylase and their preparation. And the patent contained the following:

The invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier. Compounds of formula I wherein W and Z are independently CH2 and NH and derivatives; X and Y are independently CH2, O, CO and NH and derivatives; provided that when W and Z are CH2, then WZ may be taken together with another carbon to form a bridge; R1 is H, C1-4 alkyl, (un)substituted C3-8 cycloalkyl, (un)substituted aryl, (un)substituted heterocyclyl, etc.; R2 is H and Me; R3 and R4 are independently H, OH and (un)substituted C1-4 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their HIF prolyl hydroxylase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 19.2 nM. 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 quinolinecarboxamidoacetic acid preparation hif prolyl hydroxylase inhibitor, 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.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On June 21, 2012, Surman, Matthew D.; Guzzo, Peter R.; Freeman, Emily; Henderson, Alan J. published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of tetrahydro-azacarboline MCH-1 antagonists. And the patent contained the following:

The present invention relates to tetrahydro-azacarboline derivatives I [G = NR8CR9C10 or CR9R10NR8; X = CR16, C(R16)2, N, NR16; Y = CR16, C, N; W = C or N; Q = C or N; Z = C, CH or N; L = (CH2)pO, (CH2)p, CH:CH, a bond; A = C, CH, CH2, N; B = (un)substituted (hetero)aryl, heterocyclyl, cycloalkyl; R1 = H, alkyl, cycloalkyl, etc.; R2-R5, R9-R10 = H, halo, alkyl, etc.; R6 = H, halo, aryl, etc.; R7 = H, halo, CN, etc.; R8 = H, alkyl, cycloalkyl, etc.; n = 0-3; p = 1-4] which are melanin-concentrating hormone (MCH-1) receptor antagonists. Twenty-eight compounds I were prepared E.g., a multi-step synthesis of II.HCl, starting from 2,6-dibromopyridine, was described. Exemplified compounds I were tested in the human MCH-1 binding assay (data given). The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof. 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 azacarboline preparation melanin concentrating hormone mch1 receptor antagonist, 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.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Grabowski, James Francis, Jr.; Freeman, Emily Elizabeth published a patent.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of azinone-substituted azepinoindole derivatives as MCH-1 receptor antagonists and use in the treatment of diseases. And the patent contained the following:

Title compounds I [A = CH, C, or N; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR18, C(R18)2, N, or NR18; Y = CR18, C, or N; Z = CH, C, or N; R1 = H, (un)substituted alkyl, cycloalkyl, heteroaryl, etc; R2 – R5 and R9 – R12 independently = H, halo, NH2 and derivatives, NHCO2H and derivatives, etc.; each R6 independently = H, halo, OH and derivatives, NH2 and derivatives, etc.; R7 = H, halo, NHCO2H and derivatives, (un)substituted aryl, heteroaryl, etc.; R8 = H, (un)substituted alkyl, cycloalkyl, heteroaryl, etc.; R13 and R14 independently = H, alkyl, haloalkyl, cycloalkyl, etc.; R18 = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc.; G = NR8CR9R10CR11R12, CR9R10NR8CR11R12, or CR9R10CR11R12NR8; provided that when G = CR9R10NR8CR11R12, R2 and R3 are not CONR13R14; n = 0 to 3; 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·2HCl was prepared by cross-coupling of 2-bromo-5-trifluoromethylpyridine with 2-methoxy-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine followed by demethylation, arylation with tert-Bu 8-bromo-6-methyl-1,2,4,5-tetrahydroazepino[4,5-b]indole-3(6H)-carboxylate, hydrolysis, and addition of hydrochloric acid. Select I were evaluated for their MCH-1 antagonistic activity, e.g., II·2HCl demonstrated a Ki value of 10.1 nM. 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 azinone azepinoindole derivative preparation mch receptor antagonist treatment disease, 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.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 6, 2011, Guzzo, Peter R.; Surman, Matthew David; Henderson, Alan John; Hadden, Mark; Freeman, Emily Elizabeth published a patent.Product Details of 386704-04-7 The title of the patent was Preparation of (azabicycloalkyl)indole and (azabicycloalkyl)pyrrolopyridine derivatives 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; D = NR2; R2 = H, (un)substituted alkyl, alkynyl, aryl, etc.; each R3 independently = H, halo, NH2 and derivatives, (un)substituted heteroaryl, etc; R4 = H, halo, NH2 and derivatives, (un)substituted alkyl, aryl, etc; A = (CH)n; B = (un)substituted aryl, heteroaryl, cycloalkyl, etc.; L = (CH2)pO, (CH2)p, CH=CH, or bond; X = CR10, C(R10)2, N, or NR10; Y = CR10, C, or N; Z = CH, C, or N; R10 = H, halo, (un)substituted alkyl, cycloalkyl, heteroaryl, 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·2HCl was prepared by cross-coupling of 2-bromo-2-trifluoromethylpyridine with 2-methoxy-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine followed by demethylation, arylation with tert-Bu 3-bromo-5-methyl-5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indole-11-carboxylate, hydrolysis, and addition of hydrochloric acid. Select I were evaluated for their MCH-1 antagonistic activity, e.g., II·2HCl demonstrated a Ki value of 6.5 nM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Product Details of 386704-04-7

The Article related to azabicycloalkane indole derivative preparation mch1 receptor antagonist treatment disease, 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.Product Details of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On June 30, 2020, Sahoo, Apurba Ranjan; Lalitha, Gummidi; Murugesh, V.; Bruneau, Christian; Sharma, Gangavaram V. M.; Suresh, Surisetti; Achard, Mathieu published an article.HPLC of Formula: 111-29-5 The title of the article was Direct Access to (±)-10-Desbromoarborescidine A from Tryptamine and Pentane-1,5-diol. And the article contained the following:

A single step synthetic strategy for (±)10-desbromoarborescidine A is described. Starting from tryptamine and pentane-1,5-diol, this acceptorless dehydrogenative condensation process is efficiently catalyzed by a ruthenium complex featuring proton-responsive phosphine-pyridone ligand. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).HPLC of Formula: 111-29-5

The Article related to desbromoarborescidine a preparation, tryptamine pentanediol dehydrogenative condensation ruthenium complex phosphine pyridone catalyst, 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.HPLC of Formula: 111-29-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On June 21, 2007, Vanotti, Ermes; Forte, Barbara; Martina, Katia; Menichincheri, Maria; Cirla, Alessandra; Orsini, Paolo published a patent.HPLC of Formula: 87674-15-5 The title of the patent was Preparation of heteroarylpyrrolopyridinones active as kinase inhibitors. And the patent contained the following:

The title compounds I [A = pyridin-4-yl, 3-fluoropyridin-4-yl, 2-aminopyrimidin-4-yl; R1 = H, halo, alkyl; R2 = H, alkyl, cycloalkyl, etc.; R3-R6 = H, haloalkyl, polyfluorinated alkyl, etc.; and their pharmaceutically acceptable salts] that are effective in antagonizing activity toward Cdk2 or Cdc7, were prepared Over twenty compounds I were prepared Thus, reacting tert-Bu DL-6-(3-aminopropyl)-4-oxo-2-(pyridin-4-yl)-1,4,6,7-tetrahydropyrrolo[3,2-c]pyridine-5-carboxylate with 2-methylpropionaldehyde in the presence of sodium cyanoborohydride followed by deprotection afforded DL-6-(3-isobutylaminopropyl)-2-(pyridin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one as dihydrochloride. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).HPLC of Formula: 87674-15-5

The Article related to heteroarylpyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor, heteroaryl pyrrolopyridinone preparation cdk2 cdc7 protein kinase inhibitor, 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.HPLC of Formula: 87674-15-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts