Triethylamine → N-methoxyacetyl-2-(3,4-dichlorophenyl)-4-(tetrahydropyran-2-yloxy)butylamin

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of 8.6 g of 2-(3,4-dichlorophenyl)-4-(tetrahydropyran-2-yloxy)butylamine (obtained according to PREPARATION (I), step (b)), 2.46 g of methoxyacetic acid, 5.55 g of triethylamine in 50 ml of dichloromethane is cooled to 0° C. and 14.5 g of BOP is added thereto. The reaction mixture is stirred for one hour at room temperature and concentrated under vacuum. The residue is taken up in ethyl acetate and is successively washed with water, dried over Na2SO4 and concentrated under vacuum. The residue is chromatographed on silica gel using CH2Cl2 /CH3OH (100/1 v/v) as the eluent to give 7.5 g of the expected product.

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