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US 4,380,635 AGranted
Synthesis of acylated benzothiophenes
AssigneeEli Lilly and Company
InventorMary K. Peters
Life of this patent
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Abstract
A group of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)benzoyl]benzo[b]thiophen es are prepared by acylation of a methyl-protected starting compound followed by demethylation in a single reaction mixture.
Claims13
A process for preparing a compound of the formula ##STR4## wherein R.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.4 alkyl, or combine to form C.sub.4 -C.sub.6 polymethylene, --CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.2 -- or --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 --;
- which process comprises acylating a compound of the formula ##STR5## in the presence of aluminum chloride or aluminum bromide with an acylating agent of the formula ##STR6## wherein R.sup.4 is chloro or bromo;
- and adding to the reaction mixture a sulfur compound chosen from the group consisting of methionine and compounds of the formula
- X--S--Y
- wherein X is hydrogen or unbranched C.sub.1 -C.sub.4 alkyl, and Y is C.sub.1 -C.sub.4 alkyl or phenyl.
1 more element
Dependencies are inferred from the claim text.