PRODUCTION OF HYDROXYTHIOACETAMIDES AND USE THEREOF IN THE SYNTHESIS OF BENZOTHIOPHENES

A group of 2-amino-3-aroyl-benzo[ beta ]thiophenes are prepared by preparing an alpha -hydroxy thioacetamide by silyl mediated condensation of an aldehyde with an anion of dialkylamino thioformamide, cyclizing the alpha -hydroxy thioamide, and subsequently acylating the benzo[ beta ]thiophene to yie...

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Bibliographische Detailangaben
1. Verfasser: GODFREY, ALEXANDER, GLENN
Format: Patent
Sprache:eng
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Zusammenfassung:A group of 2-amino-3-aroyl-benzo[ beta ]thiophenes are prepared by preparing an alpha -hydroxy thioacetamide by silyl mediated condensation of an aldehyde with an anion of dialkylamino 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-piperidinoethoxy)benzoyl]benzo[ beta ]thiophene.