Category: 754230-78-9

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.754230-78-9, name is 3-(Benzyloxy)-5-bromopyridin-2-amine, molecular formula is C12H11BrN2O, molecular weight is 279.13, as common compound, the synthetic route is as follows.category: pyridine-derivatives

To a solution of 3-benzyloxy-5-bronio-pyridin-2-ylamine (278 mg, 1.00 mmol) in propionitrile (24 mL) and DMF (6 mL) were added iV-methyl-7^-(3-methyl-benzofuran-2- ylmethyl)acrylamide ( 252 mg, 1.10 mmol), (/-Pr)2EtN (0.35 mL, 2.00 mmol), Pd(OAc)2 (22 mg, 0.10 mmol) and P(o-tol)3 (61 mg, 0.20 mmol), and the mixture was de-oxygenated with argon for 15 min. The mixture was heated to reflux overnight, allowed to cool, filtered through a pad of diatomaceous earth, and the filtrate was concentrated. Purification by column chromatography (silica gel, CH2Cl2ZMeOH, 96:4) and then by slow precipitation fromCH?Cfe/hexanes gave the title compound (165 mg, 39%) as a pale yellow solid and as a mixture of amide rotamers: 1H NMR (300 MHz, DMSO-^5) delta 7.77 (s, IH), 7.58-6.94 (m, 12H), 6.27 (s, 2H), 5.19 (s, 2H), 5.00-4.78′ (ms 2H), 3.18-2.92 (m, 3H), 2.27 (s, 3H); MS (ESI) m/e 428 (M + H)+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,754230-78-9, 3-(Benzyloxy)-5-bromopyridin-2-amine, and friends who are interested can also refer to it.

Reference:
Patent; AFFINIUM PHARMACEUTICALS, INC.; WO2007/67416; (2007); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 754230-78-9, name is 3-(Benzyloxy)-5-bromopyridin-2-amine. This compound has unique chemical properties. The synthetic route is as follows. Safety of 3-(Benzyloxy)-5-bromopyridin-2-amine

Under argon, 200 g (0.72 mol) of 3-(benzyloxy)-5-bromopyridine-2-amine from Example 1 6A, 590 g (3.58 mol) of ethyl 2-chloroacetoacetate and 436 g of 3 Amolecular sieve were suspended in 6 1 of ethanol, and the suspension was stirred at reflux for 72 h. The reaction mixture was filtered oil through silica gel and concentrated. The residue was purified by silica gel chromatography (petroleum ether:ethyl acetate=9: 1, then 6:4) and the product fractions were concentrated. This gave 221 g (79% of theory) of the target compound.10595] LC-MS (Method 16): R=1.31 mm10596] MS (ESpos): mlz=389 (M+H)j0597] ?H-NMR (400 MHz, DMSO-d5): oe=1.36 (t, 3H), 2.58 (s, 3H), 4.32-4.41 (m, 2H), 5.33 (s, 2H), 7.28-7.32 (m, 1H), 7.36-7.47 (m, 3H), 7.49-7.54 (m, 2H), 8.98 (d, 1H).

With the rapid development of chemical substances, we look forward to future research findings about 754230-78-9.

Reference:
Patent; Bayer Pharma Aktiengesellschaft; VAKALOPOULOS, Alexandros; GROMOV, Alexey; FOLLMANN, Markus; BROCKSCHNIEDER, Damian; STASCH, Johannes-Peter; MARQUARDT, Tobias; TERSTEEGEN, Adrian; WUNDER, Frank; REDLICH, Gorden; LANG, Dieter; LI, Volkhart Min-Jian; (95 pag.)US2016/347770; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 754230-78-9 ,Some common heterocyclic compound, 754230-78-9, molecular formula is C12H11BrN2O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Example 85A Ethyl 8-(benzyloxy)-6-bromo-2-methylimidazo[1,2-a]pyridine-3-carboxylate Under argon, 200 g (0.72 mol) of 3-(benzyloxy)-5-bromopyridine-2-amine Example 84A, 590 g (3.58 mol) of ethyl 2-chloroacetoacetate and 436 g 3 A molecular sieve were suspended in 6 l of ethanol and boiled at reflux for 72 h. The reaction mixture was filtered off through kieselguhr and concentrated. The residue was purified by silica gel chromatography (petroleum ether:ethyl acetate 9:1, then 6:4) and the product fractions were concentrated. This gave 221 g (79% of theory) of the target compound. LC-MS (Method 17): Rt=1.31 min MS (ESpos): m/z=389 (M+H)+ 1H NMR (400 MHz, DMSO-d6): delta=1.36 (t, 3H), 2.58 (s, 3H), 4.32-4.41 (m, 2H), 5.33 (s, 2H), 7.28-7.32 (m, 1H), 7.36-7.47 (m, 3H), 7.49-7.54 (m, 2H), 8.98 (d, 1H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,754230-78-9, its application will become more common.

Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; VAKALOPOULOS, Alexandros; HARTUNG, Ingo; FOLLMANN, Markus; JAUTELAT, Rolf; STRAUB, Alexander; HAssFELD, Jorma; LINDNER, Niels; SCHNEIDER, Dirk; WUNDER, Frank; STASCH, Johannes-Peter; REDLICH, Gorden; LI, Volkhart Min-Jian; BECKER-PELSTER, Eva Maria; KNORR, Andreas; US2014/128386; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem