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US 6,472,531 B1Granted
Synthesis of 3-[4-(2-aminoethoxy)-benzoyl]-2-aryl-6-hydroxybenzo[b]thiophenes
AssigneeEli Lilly and Company
InventorsElizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
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Abstract
The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
Claims5
A process for preparing a compound of the formula:
- comprising acylating a benzothiophene of the formula:
- wherein:
- R4 is C1-C4 alkoxy;
- and
- R5 is C1-C4 alkyl;
- with an acylating agent of the formula:
- wherein:
- R6 is chloro, bromo, or hydroxyl;
- in the presence of a solvent and boron trichloride.
6 more elements
Dependencies are inferred from the claim text.