Claims for Patent: 5,466,810

Summary for Patent: 5,466,810

Title:	2-amino-3-aroyl-benzo[β]thiophenes and methods for preparing and using same to produce 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[β]thiophenes
Abstract:	A group of 2-amino-3-aroyl-benzo[β]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the α-hydroxy thioamide, and subsequently acylating the benzo[β]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.
Inventor(s):	Alexander G. Godfrey
Assignee:	Eli Lilly and Co
Application Number:	US08/257,859
Patent Claims:	1. A compound of the formula: ##STR8## or pharmaceutically acceptable salts thereof; wherein R represents C1 -C6 alkyl;R" represents C1 -C6 alkyl or --(CH2)n N(R1)(R2) where n is an integer of 1 to 4, and R1 and R2 are independently C1 -C6 alkyl, or R1 and R2 combine to form C4 -C6 polymethylene or --(CH2)2 O(CH2)2 --; and R3 and R4 are independently C1 -C6 alkyl or combine to form C4 -C6 polymethylene. 2. A compound according to claim 1, wherein R represents methyl. 3. A compound according to claim 1, wherein R" is --(CH2)n NR1 R2 and n is 2. 4. A compound according to claim 1, wherein R3 and R4 are methyl. 5. A compound according to claim 3, wherein R1 and R2 together represent pentamethylene. 6. A compound according to claim 5, wherein R3 and R4 are methyl. 7. A compound according to claim 1, which is 6-methoxy-2-dimethylamino-3-[4-(2-piperidinoethoxy)benzoyl]benzo[β]thiophene.