2-Methyl-3-amino-4-acetylanisole

To a solution of 2-methyl-3-(methyloxy)aniline (5.0 g, 36.5 mmol) in p-xylene (80 mL) and cooled to 0° C., added BClStep 3: synthesis of (2-amino-4-methoxy-3-methylphenyl)(methyl)ketone (4). A solution Of BClStep 3: synthesis of (2-amino-4-methoxy-3-methylphenyl)(methyl)ketone (4); A solution Of BClPreparation of 2-Methyl-3-methoxy-6-acetyl-aniline Step E: Synthesis of l-(2-Amino-4-methoxy-3-methyl-phenyl)-ethanone (34); EPO Examples; The following examples are intended to illustrate the present invention and not to limit it thereto. EPO To a stirred solution of 4-(trifluoromethyl)-1, 3-thiazole-2-carboxylic acid (3.5 g, 1 eq.) in DCM (35 mL) at 0 C under nitrogen was added anhydrous DMF (few drops) and oxalyl chloride (3.14 mL, 2 eq.). At the end of the gas evolution, the reaction mixture was allowed to warm up to room temperature. The mixture was stirred at room temperature for 2 hrs and was evaporated. Dioxane (70 mL) was added under nitrogen followed by a solution of Added to the reaction vial 15.0g compound of formula IV, 0.1gDMF and 150 ml dichloromethane, stirring, cooling to 0-10C, dropwise 20.0g oxalyl, completion of the dropping, temperature control 15-20 C stirring 16h.Concentrating the reaction liquid dry, then adding 200mlTHF continue to concentrate under reduced pressure. Concentrated end, adding 100mlTHF, 0 . 2g4-dimethylaminopyridine (DMAP), 7.6gNa2C O3, then instillment type THF solution of compound VI (12.9g compound in formula VI 50mlTHF), completion of the dropping, the temperature rising to 30-35 C reaction 5-6 hours.Through the column chromatography purification of the product is subjected to purification, the compounds of formula II by yellow solid 15.5g, to yield 65.6%, purity of 96.7%.

Molecular Weight:179.22
XLogP3:1.8
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:179.094628657
Monoisotopic Mass:179.094628657
Topological Polar Surface Area:52.3
Heavy Atom Count:13
Complexity:193
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes