Tag: M.W:100-200

Application of 33024-60-1. Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 33024-60-1, Name is Tetrahydro-2H-pyran-4-amine hydrochloride. In a document type is Article, introducing its new discovery.

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2

Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant melanoma, but resistance frequently emerges, often mediated by increased signaling through ERK1/2. Here, we describe the fragment-based generation of ERK1/2 inhibitors that block catalytic phosphorylation of downstream substrates such as RSK but also modulate phosphorylation of ERK1/2 by MEK without directly inhibiting MEK. X-ray crystallographic and biophysical fragment screening followed by structure-guided optimization and growth from the hinge into a pocket proximal to the C-alpha helix afforded highly potent ERK1/2 inhibitors with excellent kinome selectivity. In BRAF mutant cells, the lead compound suppresses pRSK and pERK levels and inhibits proliferation at low nanomolar concentrations. The lead exhibits tumor regression upon oral dosing in BRAF mutant xenograft models, providing a promising basis for further optimization toward clinical pERK1/2 modulating ERK1/2 inhibitors.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Related Products of 2081-44-9. Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 2081-44-9, Name is Tetrahydro-2H-pyran-4-ol. In a document type is Patent, introducing its new discovery.

2. 4, 6 – tri-substituted pyrido [3, 4 – d] pyrimidine compounds and salts thereof and application (by machine translation)

The present invention provides a 2, 4, 6 – tri-substituted pyrido [3, 4 – d] pyrimidine compounds and salts thereof and application, which belongs to the technical field of anti-cancer drugs. The compounds of novel structure, easy to synthesize, inhibit epidermal growth factor receptor (EGFR) tyrosine kinase activity, for single-mutation (L858R) and double-mutant EGFR (L858R/T790M) of obvious inhibiting activity, has obvious in vivo, and outer tumor activity, with the EGFR mutation can be used for the treatment of cancers, but also its synthetic raw materials, synthetic method is easy to realize. (by machine translation)

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Application of 19752-84-2, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 19752-84-2, C5H10O2. A document type is Article, introducing its new discovery.

Hydroboration. 71. Hydroboration of Representative Heterocyclic Olefins with Borane-Methyl Sulfide, 9-Borabicyclo<3.3.1>nonane, Dicyclohexylborane, and Disiamylborane. Synthesis of Heterocyclic Alcohols

The hydroboration of representative heterocycles bearing an endocyclic double bond with borane-methyl sulfide (BMS), 9-borabicyclo<3.3.1>nonane (9-BBN), dicyclohexylborane (Chx2BH), and disiamylborane (Sia2BH) was investigated systematically to establish the optimum conditions for the clean and quantitative hydroboration.The hydroboration of 2,3- and 2,5-dihydrofurans with BMS (3:1 molar ratio) at 25 deg C for 1 h affords the trialkylborane, readily oxidized to 3-hydroxytetrahydrofuran in excellent yield.However, preparation of the corresponding dialkylboranes from these olefins using 2 olefin/BMS was not possible even at 0 deg C.Excess hydride and prolongated reaction time cause ring cleavage of the alkylboranes to yield both unsaturated alcohol and the dihydroborated products 1,3- and 1,4-pentanediols.Hydroboration of both 2,3-dihydrothiophene and 2-methyl-4,5-dihydrofuran with BMS proceeds cleanly to the trialkylborane stage, oxidized to the corresponding alcohols in almost quantitative yields.Hydroboration of 3-pyrroline with BMS could not be achieved with the unprotected nitrogen atom.Such hydroboration could be accomplished by protecting the nitrogen atom with the benzyloxycarbonyl group affording the trialkylborane, readily converted to N-(benzyloxycarbonyl)-3-pyrrolidinol in good yield.Conditions for a clean hydroboration of these heterocyclic five-membered olefins with 9-BBN, Chx2BH, and Sia2BH were also established.In all cases clean trialkylboranes were obtained, readily oxidized to heterocyclic alcohols in high yields. 3,4-Dihydropyran, on hydroboration with BMS, followed by oxidation, affords 3-hydroxytetrahydropyran in good yield.However, ring cleavage in this case is greater when compared to 2,3-dihydrofuran. 2-Methoxy- or 2-ethoxy-3,4-dihydro-2H-pyran readily undergo hydroboration with BMS to the trialkylboranes, oxidized to the corresponding trans and cis alcohols in a 7:3 ratio.As the steric requirements of the dialkylborane are increased, more trans alcohol is formed.Thus at 0 deg C, the ratios of trans to cis alcohols were increased from 1:1 to 7:3 and then to 8:2 with 9-BBN, Chx2BH, and Sia2BH, respectively.N-(Benzyloxycarbonyl)-1,2,3,6-tetrahydropyridine is readily hydroborated with BMS, 9-BBN, Chx2BH, and Sia2BH to the corresponding trialkylboranes, readily oxidized to N-(benzyloxycarbonyl)-3- and -4-piperidinols in good yield.Strongly basic groups in the heterocyclic ring can greatly reduce the ease of hydroboration, and the introduction of boron beta to the heteroatom can lead to elimination.However, both problems can be avoided to provide ready hydroboration-oxidation of heterocyclic olefins.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Application of 40191-32-0, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 40191-32-0, Name is Tetrahydro-2H-pyran-4-carbonyl chloride, molecular formula is C6H9ClO2. In a Patent£¬once mentioned of 40191-32-0

INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o-O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o-S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o-S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer’s disease, autism, Parkinson’s disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 40191-32-0 is helpful to your research., Application of 40191-32-0

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.50675-18-8, Name is Tetrahydropyran-4-carbaldehyde, molecular formula is C6H10O2. In a Patent£¬once mentioned of 50675-18-8, Computed Properties of C6H10O2

ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

Disclosed herein are substituted hexahydro-lH-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Computed Properties of C6H10O2, you can also check out more blogs about50675-18-8

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.134419-59-3, Name is Tetrahydro-2H-pyran-4-yl methanesulfonate, molecular formula is C6H12O4S. In a Patent£¬once mentioned of 134419-59-3, Application In Synthesis of Tetrahydro-2H-pyran-4-yl methanesulfonate

PROCESS FOR PRODUCTION OF 4-AMINOTETRAHYDROPYRANS AND SALTS THEREOF WITH ACIDS, INTERMEDIATES FOR THE PROCESS, AND PROCESS FOR PRODUCTION THEREOF

The present invention relates to a process for preparing 4-aminotetrahydropyran compound and an acid salt thereof represented by the formula (2):wherein R represents a hydrogen atom or a hydrocarbon group,which comprises subjecting a 4-hydrazinotetrahydropyran compound or an acid salt thereof represented by the formula (1) :wherein R has the same meaning as defined above, to decomposition reaction in the presence of at least one compound selected from Raney nickel, noble metal catalyst and metal oxide, and a synthetic intermediate thereof and a process for preparing the same.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 134419-59-3 is helpful to your research., Application In Synthesis of Tetrahydro-2H-pyran-4-yl methanesulfonate

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.50675-18-8, Name is Tetrahydropyran-4-carbaldehyde, molecular formula is C6H10O2. In a Patent£¬once mentioned of 50675-18-8, 50675-18-8

ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

Disclosed herein are substituted hexahydro-lH-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.50675-18-8, you can also check out more blogs about50675-18-8

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

19752-84-2, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 19752-84-2, C5H10O2. A document type is Article, introducing its new discovery.

Hydroboration. 71. Hydroboration of Representative Heterocyclic Olefins with Borane-Methyl Sulfide, 9-Borabicyclo<3.3.1>nonane, Dicyclohexylborane, and Disiamylborane. Synthesis of Heterocyclic Alcohols

The hydroboration of representative heterocycles bearing an endocyclic double bond with borane-methyl sulfide (BMS), 9-borabicyclo<3.3.1>nonane (9-BBN), dicyclohexylborane (Chx2BH), and disiamylborane (Sia2BH) was investigated systematically to establish the optimum conditions for the clean and quantitative hydroboration.The hydroboration of 2,3- and 2,5-dihydrofurans with BMS (3:1 molar ratio) at 25 deg C for 1 h affords the trialkylborane, readily oxidized to 3-hydroxytetrahydrofuran in excellent yield.However, preparation of the corresponding dialkylboranes from these olefins using 2 olefin/BMS was not possible even at 0 deg C.Excess hydride and prolongated reaction time cause ring cleavage of the alkylboranes to yield both unsaturated alcohol and the dihydroborated products 1,3- and 1,4-pentanediols.Hydroboration of both 2,3-dihydrothiophene and 2-methyl-4,5-dihydrofuran with BMS proceeds cleanly to the trialkylborane stage, oxidized to the corresponding alcohols in almost quantitative yields.Hydroboration of 3-pyrroline with BMS could not be achieved with the unprotected nitrogen atom.Such hydroboration could be accomplished by protecting the nitrogen atom with the benzyloxycarbonyl group affording the trialkylborane, readily converted to N-(benzyloxycarbonyl)-3-pyrrolidinol in good yield.Conditions for a clean hydroboration of these heterocyclic five-membered olefins with 9-BBN, Chx2BH, and Sia2BH were also established.In all cases clean trialkylboranes were obtained, readily oxidized to heterocyclic alcohols in high yields. 3,4-Dihydropyran, on hydroboration with BMS, followed by oxidation, affords 3-hydroxytetrahydropyran in good yield.However, ring cleavage in this case is greater when compared to 2,3-dihydrofuran. 2-Methoxy- or 2-ethoxy-3,4-dihydro-2H-pyran readily undergo hydroboration with BMS to the trialkylboranes, oxidized to the corresponding trans and cis alcohols in a 7:3 ratio.As the steric requirements of the dialkylborane are increased, more trans alcohol is formed.Thus at 0 deg C, the ratios of trans to cis alcohols were increased from 1:1 to 7:3 and then to 8:2 with 9-BBN, Chx2BH, and Sia2BH, respectively.N-(Benzyloxycarbonyl)-1,2,3,6-tetrahydropyridine is readily hydroborated with BMS, 9-BBN, Chx2BH, and Sia2BH to the corresponding trialkylboranes, readily oxidized to N-(benzyloxycarbonyl)-3- and -4-piperidinols in good yield.Strongly basic groups in the heterocyclic ring can greatly reduce the ease of hydroboration, and the introduction of boron beta to the heteroatom can lead to elimination.However, both problems can be avoided to provide ready hydroboration-oxidation of heterocyclic olefins.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

40191-32-0, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 40191-32-0, Name is Tetrahydro-2H-pyran-4-carbonyl chloride, molecular formula is C6H9ClO2. In a Patent£¬once mentioned of 40191-32-0

INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o-O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o-S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o-S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer’s disease, autism, Parkinson’s disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 40191-32-0 is helpful to your research., 40191-32-0

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.134419-59-3, Name is Tetrahydro-2H-pyran-4-yl methanesulfonate, molecular formula is C6H12O4S. In a Patent£¬once mentioned of 134419-59-3, 134419-59-3

PROCESS FOR PRODUCTION OF 4-AMINOTETRAHYDROPYRANS AND SALTS THEREOF WITH ACIDS, INTERMEDIATES FOR THE PROCESS, AND PROCESS FOR PRODUCTION THEREOF

The present invention relates to a process for preparing 4-aminotetrahydropyran compound and an acid salt thereof represented by the formula (2):wherein R represents a hydrogen atom or a hydrocarbon group,which comprises subjecting a 4-hydrazinotetrahydropyran compound or an acid salt thereof represented by the formula (1) :wherein R has the same meaning as defined above, to decomposition reaction in the presence of at least one compound selected from Raney nickel, noble metal catalyst and metal oxide, and a synthetic intermediate thereof and a process for preparing the same.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 134419-59-3 is helpful to your research., 134419-59-3

Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics