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ChemicalBook CAS DataBase List METHYL 2-CHLORO-3-NITROBENZOATE
53553-14-3

METHYL 2-CHLORO-3-NITROBENZOATE synthesis

8synthesis methods
-

Yield: 100%

Reaction Conditions:

Stage #1:2-chloro-3-nitrobezoic acid with oxalyl dichloride;N,N-dimethyl-formamide in dichloromethane at 0 - 20; for 6 h;
Stage #2:methanol in dichloromethane

Steps:

22.i
A suspension of 2-chloro-3-nitrobenzic acid (20 g, 99 mmol) in dichloromethane (800 inL) was cooled in an ice bath. Dimethylformamide (0.40 inL) was added to the reaction mixture followed by a dropwise addition of oxalyl chloride (13.85 g, 109 mmol). The reaction mixture was allowed to warm to room temperature and stirred for 6 h. Methanol(200 mL) was added dropwise to the reaction mixture and the reaction mixture was stirred overnight. The reaction mixture was concentrated in vacuo, and the residue was dissolved in dichloromethane and passed through a plug of silica eluting with a 50% ethyl acetate/n-hexanes mixture. The filtrate was concentrated in vacuo to give the title compound (21.5 g, 100%). 1H NMR (CDCl3) δ 3.98 (s, 3H), 7.48 (t, J = 7.8 Hz, IH), 7.84 (d, J = 8.2 Hz, IH), 7.95 (d, J = 7.8 Hz, IH).

References:

TAKEDA PHARMACEUTICAL COMPANY LIMITED WO2008/51533, 2008, A2 Location in patent:Page/Page column 95

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