Archives for Chemistry Experiments of 1228185-09-8

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Safety of 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, is researched, Molecular C27H36Cl2N2, CAS is 1228185-09-8, about Norbornene polymerization and copolymerization with 1-alkenes by neutral palladium complexes bearing aryloxide imidazolin-2-imine ligand. Author is Li, Mingyuan; Zhang, Hu; Cai, Zhengguo; Eisen, Moris S..

A series of novel aryloxide imidazolin-2-imine bidentate neutral Pd(II) complexes with different substituents on the imidazolin-2-imine ligand were synthesized and characterized. In the single crystal X-ray diffraction anal., the complexes Pd1 and Pd2 adopted almost square-planar geometries, while Pd3 bearing the bulkier 2,6-bis(diphenylmethyl)-4-methylphenyl substituent was obtained as the allyl adducted base-free η3 coordination mode. In the presence of very low EtAlCl2 loadings (100 equivalent), these Pd(II) complexes exhibited high activity (∼106 g mol-1 h-1) and good thermal stability (up to 100°C) toward the addition polymerization of norbornene. Most importantly, these Pd(II) catalysts were able to promote the copolymerization of norbornene with 1-dodecene and 1-octadecene with high activity (>105 g mol-1 h-1) to yield high-mol.-weight (Mn up to 5.59 x 104 g mol-1) copolymers. The 1-alkene incorporation of resulting copolymers was modulated in a wide range (5.1-15.3%) by changing the comonomer feed ratio, accompanied by the control of the glass transition temperature (Tg = 231.6-309.6°C). These complexes are rare examples of neutral Pd(II) complexes toward the efficient synthesis of norbornene-based cyclic olefin copolymers (COCs).

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, ACS Chemical Neuroscience called Translation of HDAC6 PET Imaging Using [18F]EKZ-001-cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates, Author is Celen, Sofie; Rokka, Johanna; Gilbert, Tonya M.; Koole, Michel; Vermeulen, Isabeau; Serdons, Kim; Schroeder, Frederick A.; Wagner, Florence F.; Bleeser, Tom; Hightower, Baileigh G.; Hu, Jiyun; Rahal, Dania; Beyzavi, Hudson; Vanduffel, Wim; Van Laere, Koen; Kranz, Janice E.; Hooker, Jacob M.; Bormans, Guy; Cawthorne, Christopher J., which mentions a compound: 1228185-09-8, SMILESS is CC(C1=C([N+]2=C(Cl)N(C3=C(C(C)C)C=CC=C3C(C)C)C=C2)C(C(C)C)=CC=C1)C.[Cl-], Molecular C27H36Cl2N2, Recommanded Product: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride.

Histone deacetylase 6 (HDAC6) is a multifunctional cytoplasmic enzyme involved in diverse cellular processes such as intracellular transport and protein quality control. Inhibition of HDAC6 can alleviate defects in cell and rodent models of certain diseases, particularly neurodegenerative disorders, including Alzheimer’s disease and amyotrophic lateral sclerosis. However, while HDAC6 represents a potentially powerful therapeutic target, development of effective brain-penetrant HDAC6 inhibitors remains challenging. Recently, [18F]EKZ-001 ([18F]Bavarostat), a brain-penetrant positron emission tomog. (PET) radioligand with high affinity and selectivity toward HDAC6, was developed and evaluated preclinically for its ability to bind HDAC6. Herein, we describe the efficient and robust fully automated current Good Manufacturing Practices (cGMP) compliant production method. [18F]EKZ-001 quantification methods were validated in nonhuman primates (NHP) using full kinetic modeling, and [18F]EKZ-001 PET was applied to compare dose-occupancy relationships between two HDAC6 inhibitors, EKZ-317 and ACY-775. [18F]EKZ-001 is cGMP produced with an average decay-corrected radiochem. yield of 14% and an average molar activity of 204 GBq/μmol. We demonstrate that a two-tissue compartmental model and Logan graphical anal. are appropriate for [18F]EKZ-001 PET quantification in NHP brain. Blocking studies show that the novel compound EKZ-317 achieves higher target occupancy than ACY-775. This work supports the translation of [18F]EKZ-001 PET for first-in-human studies.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Name: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, is researched, Molecular C27H36Cl2N2, CAS is 1228185-09-8, about Translation of HDAC6 PET Imaging Using [18F]EKZ-001-cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates. Author is Celen, Sofie; Rokka, Johanna; Gilbert, Tonya M.; Koole, Michel; Vermeulen, Isabeau; Serdons, Kim; Schroeder, Frederick A.; Wagner, Florence F.; Bleeser, Tom; Hightower, Baileigh G.; Hu, Jiyun; Rahal, Dania; Beyzavi, Hudson; Vanduffel, Wim; Van Laere, Koen; Kranz, Janice E.; Hooker, Jacob M.; Bormans, Guy; Cawthorne, Christopher J..

Histone deacetylase 6 (HDAC6) is a multifunctional cytoplasmic enzyme involved in diverse cellular processes such as intracellular transport and protein quality control. Inhibition of HDAC6 can alleviate defects in cell and rodent models of certain diseases, particularly neurodegenerative disorders, including Alzheimer’s disease and amyotrophic lateral sclerosis. However, while HDAC6 represents a potentially powerful therapeutic target, development of effective brain-penetrant HDAC6 inhibitors remains challenging. Recently, [18F]EKZ-001 ([18F]Bavarostat), a brain-penetrant positron emission tomog. (PET) radioligand with high affinity and selectivity toward HDAC6, was developed and evaluated preclinically for its ability to bind HDAC6. Herein, we describe the efficient and robust fully automated current Good Manufacturing Practices (cGMP) compliant production method. [18F]EKZ-001 quantification methods were validated in nonhuman primates (NHP) using full kinetic modeling, and [18F]EKZ-001 PET was applied to compare dose-occupancy relationships between two HDAC6 inhibitors, EKZ-317 and ACY-775. [18F]EKZ-001 is cGMP produced with an average decay-corrected radiochem. yield of 14% and an average molar activity of 204 GBq/μmol. We demonstrate that a two-tissue compartmental model and Logan graphical anal. are appropriate for [18F]EKZ-001 PET quantification in NHP brain. Blocking studies show that the novel compound EKZ-317 achieves higher target occupancy than ACY-775. This work supports the translation of [18F]EKZ-001 PET for first-in-human studies.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Category: tetrahydropyran. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, is researched, Molecular C27H36Cl2N2, CAS is 1228185-09-8, about Translation of HDAC6 PET Imaging Using [18F]EKZ-001-cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates. Author is Celen, Sofie; Rokka, Johanna; Gilbert, Tonya M.; Koole, Michel; Vermeulen, Isabeau; Serdons, Kim; Schroeder, Frederick A.; Wagner, Florence F.; Bleeser, Tom; Hightower, Baileigh G.; Hu, Jiyun; Rahal, Dania; Beyzavi, Hudson; Vanduffel, Wim; Van Laere, Koen; Kranz, Janice E.; Hooker, Jacob M.; Bormans, Guy; Cawthorne, Christopher J..

Histone deacetylase 6 (HDAC6) is a multifunctional cytoplasmic enzyme involved in diverse cellular processes such as intracellular transport and protein quality control. Inhibition of HDAC6 can alleviate defects in cell and rodent models of certain diseases, particularly neurodegenerative disorders, including Alzheimer’s disease and amyotrophic lateral sclerosis. However, while HDAC6 represents a potentially powerful therapeutic target, development of effective brain-penetrant HDAC6 inhibitors remains challenging. Recently, [18F]EKZ-001 ([18F]Bavarostat), a brain-penetrant positron emission tomog. (PET) radioligand with high affinity and selectivity toward HDAC6, was developed and evaluated preclinically for its ability to bind HDAC6. Herein, we describe the efficient and robust fully automated current Good Manufacturing Practices (cGMP) compliant production method. [18F]EKZ-001 quantification methods were validated in nonhuman primates (NHP) using full kinetic modeling, and [18F]EKZ-001 PET was applied to compare dose-occupancy relationships between two HDAC6 inhibitors, EKZ-317 and ACY-775. [18F]EKZ-001 is cGMP produced with an average decay-corrected radiochem. yield of 14% and an average molar activity of 204 GBq/μmol. We demonstrate that a two-tissue compartmental model and Logan graphical anal. are appropriate for [18F]EKZ-001 PET quantification in NHP brain. Blocking studies show that the novel compound EKZ-317 achieves higher target occupancy than ACY-775. This work supports the translation of [18F]EKZ-001 PET for first-in-human studies.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, is researched, Molecular C27H36Cl2N2, CAS is 1228185-09-8, about Norbornene polymerization and copolymerization with 1-alkenes by neutral palladium complexes bearing aryloxide imidazolin-2-imine ligand.Recommanded Product: 1228185-09-8.

A series of novel aryloxide imidazolin-2-imine bidentate neutral Pd(II) complexes with different substituents on the imidazolin-2-imine ligand were synthesized and characterized. In the single crystal X-ray diffraction anal., the complexes Pd1 and Pd2 adopted almost square-planar geometries, while Pd3 bearing the bulkier 2,6-bis(diphenylmethyl)-4-methylphenyl substituent was obtained as the allyl adducted base-free η3 coordination mode. In the presence of very low EtAlCl2 loadings (100 equivalent), these Pd(II) complexes exhibited high activity (∼106 g mol-1 h-1) and good thermal stability (up to 100°C) toward the addition polymerization of norbornene. Most importantly, these Pd(II) catalysts were able to promote the copolymerization of norbornene with 1-dodecene and 1-octadecene with high activity (>105 g mol-1 h-1) to yield high-mol.-weight (Mn up to 5.59 x 104 g mol-1) copolymers. The 1-alkene incorporation of resulting copolymers was modulated in a wide range (5.1-15.3%) by changing the comonomer feed ratio, accompanied by the control of the glass transition temperature (Tg = 231.6-309.6°C). These complexes are rare examples of neutral Pd(II) complexes toward the efficient synthesis of norbornene-based cyclic olefin copolymers (COCs).

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride(SMILESS: CC(C1=C([N+]2=C(Cl)N(C3=C(C(C)C)C=CC=C3C(C)C)C=C2)C(C(C)C)=CC=C1)C.[Cl-],cas:1228185-09-8) is researched.SDS of cas: 97739-46-3. The article 《AlkylFluor: Deoxyfluorination of Alcohols》 in relation to this compound, is published in Organic Letters. Let’s take a look at the latest research on this compound (cas:1228185-09-8).

A practical, high-yielding method for the deoxyfluorination of alcs. is presented using AlkylFluor, a novel salt analog of PhenoFluor. AlkylFluor is readily prepared on multigram scale and is stable to long-term storage in air and exposure to water. The practicality and applicability of this method is demonstrated with a variety of primary and secondary alc. substrates.

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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics