Category: 908267-63-0

On January 29, 2015, Le Tiran, Arnaud; Le Diguarher, Thierry; Starck, Jerome-Benoit; Henlin, Jean-Michel; De Nanteuil, Guillaume; Geneste, Olivier; Davidson, James Edward Paul; Murray, James Brooke; Chen, I-Jen published a patent.Synthetic Route of 908267-63-0 The title of the patent was New indolizine carboxamide derivatives, their preparation as pro-apoptotic and antitumor agents and their pharmaceutical compositions containing them. And the patent contained the following:

Indolizine and indolizine derivatives, especially 5,6,7,8-tetrahydroindolizine optionally substituted with an NH2 group, 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine optionally substituted with a Me group and pyrrolo[1,2-a]pyrimidine derivatives, e.g., I•HCl, were prepared as inducers of caspase activity and apoptosis for treating neoplasm. Thus, I•HCl was prepared by a multi-step procedure starting from II (preparation given) and (3R)-3-methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride (preparation given). I•HCl was evaluated for its ability to induce caspase activity and therefore apoptosis in vitro and in vivo and for its ability to inhibit the Bcl-2 protein. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Synthetic Route of 908267-63-0

The Article related to indolizine preparation antitumor proapoptotic agent inducer caspase activity apoptosis, pyrrolopyrazine pyrrolopyrimidine indolizine carboxamide preparation antitumor proapoptotic agent and other aspects.Synthetic Route of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 31, 2013, Ueno, Hirokazu; Yamamoto, Takashi; Takashita, Ryuta; Yokoyama, Ryohei; Sugiura, Toshihiko; Kageyama, Shunsuke; Ando, Ayatoshi; Eda, Hiroyuki; Eviryanti, Agung; Miyazawa, Tomoko; Kirihara, Aya; Tanabe, Itsuya; Nakamura, Tarou; Noguchi, Misato; Shuto, Manami; Sugiki, Masayuki; Dohi, Mizuki published a patent.Application In Synthesis of 4-Bromo-2-isopropylpyridine The title of the patent was Preparation of N-(4-sulfonamidobenzoyl)-L-phenylalanine and N-(4-sulfonamidobenzoyl)-3-(pyridin-2-yl)-L-alanine derivatives as α4-integrin inhibitors. And the patent contained the following:

There are provided L-phenylalanine and 3-(pyridin-2-yl)-L-alanine derivatives having terminal sulfonamide groups and heterocyclic groups [I; A = Q, Q1, Q2; Arm = cycloalkane or aromatic ring containing 0-4 heteroatoms selected from O, S, and N; R1, R2, R3, R11, R12, R13, R14, R21, R22, R23, R24, R25 = group A, H, lower alkylamino, lower alkylamino-lower alkyl; group A = halo, HO, each hydroxy- or halo-(un)substituted lower alkyl, alkenyl, alkynyl, or alkylthio, NO2, NH2, CO2H, lower alkyloxycarbonyl, CONH2, lower alkanoyl, aroyl, lower alkylsulfonyl, SO2NH2, ammonium group; B = (un)substituted lower alkoxy, HO, hydroxyamino; R41 = H, lower alkyl; a, b, c, d = CR31, CR32, CR33, CR34; e, f, g, h = CR35, CR36, CR37, CR38; R31-R38 = H, halo, lower alkyl, lower alkoxy, NO2; wherein one or two of a, b, c, and d = N atom; one or two of e, f, g, and h = N atom; at least one of R31-R34 = halo or lower alkyl; D = each (un)substituted Ph or heterocyclyl; E = group A, lower alkylaminoalkylene, (un)substituted 5- or 6-membered heterocyclyl, or substituted CONH2; or lower alkylcarbonyl and lower alkyloxycarbonyl in E group are linked to Ph of D group to form a ring] or pharmaceutically acceptable salts thereof. These compounds have excellent α4-integrin-inhibiting activity with high selectivity for α4β7-integrin over α4β1-integrin. They are useful for the treatment or prevention of inflammatory diseases related to α4β7 integrin-dependent adhesion process. Thus, 100 mg Me 4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate and 89.0 mg 2,6-difluoro-4-[[[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino]benzoic acid were suspended in 2.0 mL CH2Cl2, treated with 133 mg HATU and 0.160 mL diisopropylethylamine, stirred at room temperature for 2 h, and concentrated under reduced pressure to give, after purification using reversed phase HPLC, Me N-[2,6-difluoro-4-([[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino)benzoyl]-4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate (II; R = Me) tris(trifluoroacetate). II.3CF3CO2H (R = Me) (25.0 mg) was treated with 2.0 mL 4 N HCl/dioxane solution and 2.0 mL H2O, stirred at 80° for 1 h, and concentrated to give, after purification using reversed phase HPLC, II.3CF3CO2H (R = H). II (R = H) (free base) inhibited the binding of MAdCAM to human RPMI-8866 cells expressing α4β7 integrin and that of MAdCAM to human RPMI-8866 cells expressing α4β1 integrin with IC50 of 0.060 and nM, resp., and 220-fold inhibition selectivity for α4β7 integrin. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Application In Synthesis of 4-Bromo-2-isopropylpyridine

The Article related to sulfonamidobenzoylhenylalanine preparation selective alpha 4 beta 7 integrin inhibitor, inflammatory disease treatment prevention sulfonamidobenzoylhenylalanine preparation, sulfonamidobenzoylpyridinylalanine preparation selective alpha 4 beta 7 integrin inhibitor and other aspects.Application In Synthesis of 4-Bromo-2-isopropylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 29, 2015, Basinger, Jillian; Bookser, Brett; Chen, Mi; Chung, Demichael; Gupta, Varsha; Hudson, Andrew; Kaplan, Alan; Na, James; Renick, Joel; Santora, Vincent published a patent.Related Products of 908267-63-0 The title of the patent was Preparation of substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors. And the patent contained the following:

The title compounds I [R1 = CO2H, C(O)NH2, SO2(alkyl), etc.; R2 = H, halo, alkyl, etc.; R3 = H, alkyl, haloalkyl, etc.; R4 = H, F, alkyl, etc.; R5 = alkyl, haloalkyl, alkoxy, etc.; X = (CR)1-2; R = H, alkyl], useful in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurol. disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alc.-dependence, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate and 1-fluoro-4-iodobenzene, was described. The exemplified compounds I were their GlyT1 inhibitory activity (data given). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Related Products of 908267-63-0

The Article related to pyrrolopyrazole pyrazolopyridine preparation glyt1 inhibitor neurol disorder treatment, cns agent cognition enhancer neuroprotection pyrrolopyrazole pyrazolopyridine preparation glyt1, dementia neurodegenerative disease stroke motor deficit pyrrolopyrazole pyrazolopyridine preparation and other aspects.Related Products of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rieder, Samuel; Melendez, Camilo; Denes, Fabrice; Jangra, Harish; Mulliri, Kleni; Zipse, Hendrik; Renaud, Philippe published an article in 2021, the title of the article was Radical chain monoalkylation of pyridines.SDS of cas: 908267-63-0 And the article contains the following content:

The monoalkylation of N-methoxypyridinium salts with alkyl radicals generated from alkenes (via hydroboration with catecholborane), alkyl iodides (via iodine atom transfer) and xanthates to afford alkylated quinoline derivatives R-R1 [R = 4-methylquinolinyl, 4-Cl-quinolinyl, 3-Br-quinolinyl, etc.; R1 = Et, iPr, cyclohexyl, etc.] and pyridine derivatives R2-R3 [R2 = 4-phenylpyridinyl, 4-tBu-pyridinyl, 4-Br-pyridinyl, etc.; R3 = iPr, 1-adamantyl, cyclohexyl, etc.] was reported. The reaction proceeded under neutral conditions since no acid was needed to activate the heterocycle and no external oxidant was required. A rate constant for the addition of a primary radical to N-methoxylepidinium >107 M-1 s-1 was exptl. determined This rate constant was more than one order of magnitude larger than the one measured for the addition of primary alkyl radicals to protonated lepidine demonstrating the remarkable reactivity of methoxypyridinium salts toward radicals. The reaction was used for the preparation of unique pyridinylated terpenoids and was extended to a three-component carbopyridinylation of electron-rich alkenes including enol esters, enol ethers and enamides. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).SDS of cas: 908267-63-0

The Article related to alkylated pyridine derivative preparation, pyridine derivative alkene monoalkylation, alkyl iodide pyridine derivative monoalkylation, xanthate pyridine derivative monoalkylation, derivative pyridine alkylated preparation, ester alkene pyridine derivative three component carbopyridinylation and other aspects.SDS of cas: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rieder, Samuel; Melendez, Camilo; Denes, Fabrice; Jangra, Harish; Mulliri, Kleni; Zipse, Hendrik; Renaud, Philippe published an article in 2021, the title of the article was Radical chain monoalkylation of pyridines.SDS of cas: 908267-63-0 And the article contains the following content:

The monoalkylation of N-methoxypyridinium salts with alkyl radicals generated from alkenes (via hydroboration with catecholborane), alkyl iodides (via iodine atom transfer) and xanthates to afford alkylated quinoline derivatives R-R1 [R = 4-methylquinolinyl, 4-Cl-quinolinyl, 3-Br-quinolinyl, etc.; R1 = Et, iPr, cyclohexyl, etc.] and pyridine derivatives R2-R3 [R2 = 4-phenylpyridinyl, 4-tBu-pyridinyl, 4-Br-pyridinyl, etc.; R3 = iPr, 1-adamantyl, cyclohexyl, etc.] was reported. The reaction proceeded under neutral conditions since no acid was needed to activate the heterocycle and no external oxidant was required. A rate constant for the addition of a primary radical to N-methoxylepidinium >107 M-1 s-1 was exptl. determined This rate constant was more than one order of magnitude larger than the one measured for the addition of primary alkyl radicals to protonated lepidine demonstrating the remarkable reactivity of methoxypyridinium salts toward radicals. The reaction was used for the preparation of unique pyridinylated terpenoids and was extended to a three-component carbopyridinylation of electron-rich alkenes including enol esters, enol ethers and enamides. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).SDS of cas: 908267-63-0

The Article related to alkylated pyridine derivative preparation, pyridine derivative alkene monoalkylation, alkyl iodide pyridine derivative monoalkylation, xanthate pyridine derivative monoalkylation, derivative pyridine alkylated preparation, ester alkene pyridine derivative three component carbopyridinylation and other aspects.SDS of cas: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 31, 2013, Ueno, Hirokazu; Yamamoto, Takashi; Takashita, Ryuta; Yokoyama, Ryohei; Sugiura, Toshihiko; Kageyama, Shunsuke; Ando, Ayatoshi; Eda, Hiroyuki; Eviryanti, Agung; Miyazawa, Tomoko; Kirihara, Aya; Tanabe, Itsuya; Nakamura, Tarou; Noguchi, Misato; Shuto, Manami; Sugiki, Masayuki; Dohi, Mizuki published a patent.Application In Synthesis of 4-Bromo-2-isopropylpyridine The title of the patent was Preparation of N-(4-sulfonamidobenzoyl)-L-phenylalanine and N-(4-sulfonamidobenzoyl)-3-(pyridin-2-yl)-L-alanine derivatives as α4-integrin inhibitors. And the patent contained the following:

There are provided L-phenylalanine and 3-(pyridin-2-yl)-L-alanine derivatives having terminal sulfonamide groups and heterocyclic groups [I; A = Q, Q1, Q2; Arm = cycloalkane or aromatic ring containing 0-4 heteroatoms selected from O, S, and N; R1, R2, R3, R11, R12, R13, R14, R21, R22, R23, R24, R25 = group A, H, lower alkylamino, lower alkylamino-lower alkyl; group A = halo, HO, each hydroxy- or halo-(un)substituted lower alkyl, alkenyl, alkynyl, or alkylthio, NO2, NH2, CO2H, lower alkyloxycarbonyl, CONH2, lower alkanoyl, aroyl, lower alkylsulfonyl, SO2NH2, ammonium group; B = (un)substituted lower alkoxy, HO, hydroxyamino; R41 = H, lower alkyl; a, b, c, d = CR31, CR32, CR33, CR34; e, f, g, h = CR35, CR36, CR37, CR38; R31-R38 = H, halo, lower alkyl, lower alkoxy, NO2; wherein one or two of a, b, c, and d = N atom; one or two of e, f, g, and h = N atom; at least one of R31-R34 = halo or lower alkyl; D = each (un)substituted Ph or heterocyclyl; E = group A, lower alkylaminoalkylene, (un)substituted 5- or 6-membered heterocyclyl, or substituted CONH2; or lower alkylcarbonyl and lower alkyloxycarbonyl in E group are linked to Ph of D group to form a ring] or pharmaceutically acceptable salts thereof. These compounds have excellent α4-integrin-inhibiting activity with high selectivity for α4β7-integrin over α4β1-integrin. They are useful for the treatment or prevention of inflammatory diseases related to α4β7 integrin-dependent adhesion process. Thus, 100 mg Me 4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate and 89.0 mg 2,6-difluoro-4-[[[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino]benzoic acid were suspended in 2.0 mL CH2Cl2, treated with 133 mg HATU and 0.160 mL diisopropylethylamine, stirred at room temperature for 2 h, and concentrated under reduced pressure to give, after purification using reversed phase HPLC, Me N-[2,6-difluoro-4-([[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]sulfonyl]amino)benzoyl]-4-(1-methyl-2,4-dioxo-1,4-dihydropyrido[3,4-d]pyrimidin-3(2H)-yl)-L-phenylalaninate (II; R = Me) tris(trifluoroacetate). II.3CF3CO2H (R = Me) (25.0 mg) was treated with 2.0 mL 4 N HCl/dioxane solution and 2.0 mL H2O, stirred at 80° for 1 h, and concentrated to give, after purification using reversed phase HPLC, II.3CF3CO2H (R = H). II (R = H) (free base) inhibited the binding of MAdCAM to human RPMI-8866 cells expressing α4β7 integrin and that of MAdCAM to human RPMI-8866 cells expressing α4β1 integrin with IC50 of 0.060 and nM, resp., and 220-fold inhibition selectivity for α4β7 integrin. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Application In Synthesis of 4-Bromo-2-isopropylpyridine

The Article related to sulfonamidobenzoylhenylalanine preparation selective alpha 4 beta 7 integrin inhibitor, inflammatory disease treatment prevention sulfonamidobenzoylhenylalanine preparation, sulfonamidobenzoylpyridinylalanine preparation selective alpha 4 beta 7 integrin inhibitor and other aspects.Application In Synthesis of 4-Bromo-2-isopropylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 29, 2015, Basinger, Jillian; Bookser, Brett; Chen, Mi; Chung, Demichael; Gupta, Varsha; Hudson, Andrew; Kaplan, Alan; Na, James; Renick, Joel; Santora, Vincent published a patent.Related Products of 908267-63-0 The title of the patent was Preparation of substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors. And the patent contained the following:

The title compounds I [R1 = CO2H, C(O)NH2, SO2(alkyl), etc.; R2 = H, halo, alkyl, etc.; R3 = H, alkyl, haloalkyl, etc.; R4 = H, F, alkyl, etc.; R5 = alkyl, haloalkyl, alkoxy, etc.; X = (CR)1-2; R = H, alkyl], useful in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurol. disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alc.-dependence, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate and 1-fluoro-4-iodobenzene, was described. The exemplified compounds I were their GlyT1 inhibitory activity (data given). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Related Products of 908267-63-0

The Article related to pyrrolopyrazole pyrazolopyridine preparation glyt1 inhibitor neurol disorder treatment, cns agent cognition enhancer neuroprotection pyrrolopyrazole pyrazolopyridine preparation glyt1, dementia neurodegenerative disease stroke motor deficit pyrrolopyrazole pyrazolopyridine preparation and other aspects.Related Products of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem