Category: 38186-85-5

Schrader, Thomas O. et al. published their research in ACS Medicinal Chemistry Letters in 2021 | CAS: 38186-85-5

2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5) belongs to pyridine derivatives. Pyridine has a conjugated system of six 蟺 electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H眉ckel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C鈥揌 in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Product Details of 38186-85-5

Discovery of PIPE-359, a Brain-Penetrant, Selective M1 Receptor Antagonist with Robust Efficacy in Murine MOG-EAE was written by Schrader, Thomas O.;Xiong, Yifeng;Lorenzana, Ariana O.;Broadhead, Alexander;Stebbins, Karin J.;Poon, Michael M.;Baccei, Christopher;Lorrain, Daniel S.. And the article was included in ACS Medicinal Chemistry Letters in 2021.Product Details of 38186-85-5 This article mentions the following:

The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M1 antagonist, linker replacement and structure-activity relationship investigations of the eastern 1-(pyridinyl)piperazine led to the identification of a novel, potent, and selective antagonist with good MDCKII-MDR1 permeability. Continued semi-iterative positional scanning facilitated improvements in the metabolic and hERG profiles, which ultimately delivered PIPE-359. This advanced drug candidate exhibited robust efficacy in mouse myelin oligodendrocyte glycoprotein (MOG)-induced exptl. autoimmune encephalitis (EAE), a preclin. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5Product Details of 38186-85-5).

2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5) belongs to pyridine derivatives. Pyridine has a conjugated system of six 蟺 electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H眉ckel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C鈥揌 in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Product Details of 38186-85-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Schrader, Thomas O. et al. published their research in ACS Medicinal Chemistry Letters in 2021 | CAS: 38186-85-5

2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Product Details of 38186-85-5

Discovery of PIPE-359, a Brain-Penetrant, Selective M1 Receptor Antagonist with Robust Efficacy in Murine MOG-EAE was written by Schrader, Thomas O.;Xiong, Yifeng;Lorenzana, Ariana O.;Broadhead, Alexander;Stebbins, Karin J.;Poon, Michael M.;Baccei, Christopher;Lorrain, Daniel S.. And the article was included in ACS Medicinal Chemistry Letters in 2021.Product Details of 38186-85-5 This article mentions the following:

The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M1 antagonist, linker replacement and structure-activity relationship investigations of the eastern 1-(pyridinyl)piperazine led to the identification of a novel, potent, and selective antagonist with good MDCKII-MDR1 permeability. Continued semi-iterative positional scanning facilitated improvements in the metabolic and hERG profiles, which ultimately delivered PIPE-359. This advanced drug candidate exhibited robust efficacy in mouse myelin oligodendrocyte glycoprotein (MOG)-induced exptl. autoimmune encephalitis (EAE), a preclin. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5Product Details of 38186-85-5).

2-Bromo-5-fluoro-3-methylpyridine (cas: 38186-85-5) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.Product Details of 38186-85-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The important role of 38186-85-5

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine.

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 38186-85-5, name is 2-Bromo-5-fluoro-3-methylpyridine. A new synthetic method of this compound is introduced below., COA of Formula: C6H5BrFN

a) 5-Fluoro-3-methyl-pyridine-2-carboxylic acid methyl ester To a solution of 2-bromo-5-fluoro-3-methyl-pyridine (4.90 g) in AcOEt (100 ml) and MeOH (10 ml) was subsequently added NEt3 (5.4 ml) and 1,1′-bis(diphenylphosphino) ferrocene-palladium(II)dichloride dichloromethane adduct (490 mg) and the mixture was carbonylated at 100 bar CO and 110 C. for 20 h. The mixture was evaporated and the residue purified by chromatography on silica gel using n-heptane/AcOEt (7:1) to give the title compound (3.44 g) as a pale red solid. MS: m/z=170.1 [M+H]+.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine.

Reference:
Patent; Banner, David; Guba, Wolfgang; Hilpert, Hans; Humm, Roland; Mauser, Harald; Mayweg, Alexander V.; Narquizian, Robert; Power, Eoin; Rogers-Evans, Mark; Rombach, Didier; Woltering, Thomas; Wostl, Wolfgang; US2011/312937; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The important role of 38186-85-5

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine.

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 38186-85-5, name is 2-Bromo-5-fluoro-3-methylpyridine. A new synthetic method of this compound is introduced below., COA of Formula: C6H5BrFN

a) 5-Fluoro-3-methyl-pyridine-2-carboxylic acid methyl ester To a solution of 2-bromo-5-fluoro-3-methyl-pyridine (4.90 g) in AcOEt (100 ml) and MeOH (10 ml) was subsequently added NEt3 (5.4 ml) and 1,1′-bis(diphenylphosphino) ferrocene-palladium(II)dichloride dichloromethane adduct (490 mg) and the mixture was carbonylated at 100 bar CO and 110 C. for 20 h. The mixture was evaporated and the residue purified by chromatography on silica gel using n-heptane/AcOEt (7:1) to give the title compound (3.44 g) as a pale red solid. MS: m/z=170.1 [M+H]+.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine.

Reference:
Patent; Banner, David; Guba, Wolfgang; Hilpert, Hans; Humm, Roland; Mauser, Harald; Mayweg, Alexander V.; Narquizian, Robert; Power, Eoin; Rogers-Evans, Mark; Rombach, Didier; Woltering, Thomas; Wostl, Wolfgang; US2011/312937; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The origin of a common compound about 38186-85-5

At the same time, in my other blogs, there are other synthetic methods of this type of compound,38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine, and friends who are interested can also refer to it.

Related Products of 38186-85-5, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 38186-85-5, name is 2-Bromo-5-fluoro-3-methylpyridine. A new synthetic method of this compound is introduced below.

To a solution of 2-bromo-5-fluoro-3-methyl-pyridine (4.90 g) in AcOEt (100 ml) and MeOH (10 ml) was subsequently added NEt3 (5.4 ml) and 1,1 ‘- bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane adduct (490 mg) and the mixture was carbonylated at 100 bar CO and 110C for 20 h. The mixture was evaporated and the residue purified by chromatography on silica gel using n- heptane/ AcOEt (7: 1) to give the title compound (3.44 g) as a pale red solid. MS: m/z = 170.1 [M+H]+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,38186-85-5, 2-Bromo-5-fluoro-3-methylpyridine, and friends who are interested can also refer to it.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; SIENA BIOTECH S.P.A.; BANNER, David; GUBA, Wolfgang; HILPERT, Hans; HUMM, Roland; MAUSER, Harald; MAYWEG, Alexander, V.; NARQUIZIAN, Robert; POWER, Eoin; ROGERS-EVANS, Mark; ROMBACH, Didier; WOLTERING, Thomas; WOSTL, Wolfgang; WO2011/138293; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem