2-amino-3-aroyl-benzo[ beta ]thiophenes and methods for preparing and using same to produce 6-hdyroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[ beta ]thiophenes

摘要

A group of 2-amino-3-aroyl-benzo[ beta ]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the alpha -hydroxy thioamide, and subsequently acylating the benzo[ beta ]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-peperidinoethoxy)benzoyl]benzo[ beta ]thiophene.