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886732-31-6

Methyl 3-(aminomethyl)-5-fluorobenzoate HCl synthesis

2synthesis methods
-

Yield: 94%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane;dichloromethane at 20; for 4.5 h;

Steps:

2.2.2D
To a solution of title compound 2C, 3-(tert-butoxycarbonylamino-methyl)-5-fluorobenzoic acid methyl ester, (0.41 g, 1.45 mmol) in DCM (10 ml) is added 4M HCl in dioxane (4 eq, 5.65 mmol) and the mixture is stirred at room temperature for 4.5 h. The solvents are removed in vacuo. The residue is redissolved in DCM and carbonate resin is added and the mixture is stirred at room temperature overnight. The mixture is filtered and the solvent is removed in vacuo to give the title compound (0.25 g, 94%). LC/MS: 48% MH+, m/z 184, Rt = 0.76 mins.

References:

Evotec OAI AG;DeveloGen Aktiengesellschaft EP1655283, 2006, A1 Location in patent:Page/Page column 17