C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 333/62 (2006.01) C07D 333/66 (2006.01) C07D 409/12 (2006.01)
Patent
CA 2192097
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-piperidinoethoxy)benzoyl]benzo[.beta.]thiophene.
On prépare un groupe de 2-amino-3-aroyl-benzo[.beta.]thiophènes en traitant un aldéhyde avec un anion de diméthylamino thioformamide, en cyclisant le .alpha.-hydroxy thioamide, et en acylant ensuite le benzo[.beta.]thiophène afin d'obtenir le dérivé 2-amino-3 aryle. On peut traiter ces composés avec des réactifs de Grignard phénylés appropriés, et l'on obtient, après déprotection, le 6-hydroxy-2-(4-hydroxyphényl)-3-[4-(2-pipéridinoéthoxy)benzoyl]benzo[.beta.]thiophène.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
LandOfFree
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