Synthetic Route of 109-85-3,Some common heterocyclic compound, 109-85-3, name is 2-Methoxyethylamine, molecular formula is C3H9NO, 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.
(4-Bromo-6-chloro-quinolin-2-yl)-(4-fluoro-2-methoxy-benzyl)-amine (prepared from 2-amino-6-chloro-4-hydroxyquinoline and 4-fluoro-2-methoxybenzaldehyde as described in example 30, step A and B, 328 mg, 0.828 mmol) was dissolved in 5 mL dioxane. Argon was bubbled through the solution for 2 minutes to remove oxygen. 2-Methoxyethylamine (187 mg, 2.49 mmol), sodium tert.-butylate (159 mg, 1.66 mmol), 1,1′-bis(diphenylphosphino)ferrocene (69 mg, 0.125 mmol) and 1,1′-bis(diphenylphosphino)ferrocene palladium (II) chloride (34 mg, 0.042 mmol) were added. The reaction mixture was stirred in a sealed tube at 100 C. for 2 h. The solvent was evaporated and the residue purified by flash chromatography on silica gel (dichloromethane/methanol/ammonia 100:0:0?110:10:1 gradient). 6-Chloro-N2-(4-fluoro-2-methoxy-benzyl)-N4-(2-methoxy-ethyl)-quinoline-2,4-diamine was obtained as an off-white foam (285 mg, 88%), MS: m/e=390.0 (M+H+).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Methoxyethylamine, its application will become more common.
Reference:
Patent; Kolczewski, Sabine; Riemer, Claus; Steward, Lucinda; Wichmann, Juergen; Woltering, Thomas; US2009/88451; (2009); A1;,
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