4-Nitrobenzoyl chloride → (+)-cis-2-(4-methoxyphenyl)-3-(4-nitrobenzoyloxy)-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-1,5-benzothiazepin-4(5H)-one

Participants

Reaction Steps

3.73 g of (+)-cis-2-(4-methoxyphenyl)-3-hydroxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-1,5-benzothiazepin-4(5H)-one are dissolved in 40 ml of acetone, and 2.07 g of potassium carbonate are added thereto. 2.04 g of 4-nitrobenzoyl chloride are added at room temperature to the mixture under stirring, and said mixture is stirred at the same temperature overnight. After the reaction, the mixture is treated in the same manner as described in Example 8. 3.8 g of (+)-cis-2-(4-methoxyphenyl)-3-(4-nitrobenzoyloxy)-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-1,5-benzothiazepin-4(5H)-one are obtained.

Provenance & Evidence