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US 6,388,127 B1Granted
Process for preparing cyclic thioamides
AssigneePfizer Inc.
InventorsGeorge Joseph Quallich, Jeffrey William Raggon, Paul D. Hill
Life of this patent
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Abstract
The present invention relates to a process for preparing a compound of the formula wherein b, Y and R3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic lactams and imides which are selective agonists and antagonists of serotonin 1 (5-HT1) receptors.
Claims14
A process for preparing a compound of the formula
- wherein b is 0, 1, 2 or 3;
- Y is oxygen, sulfur, NH or N-acetyl;
- and each R3 is independently selected from the group consisting of halo, cyano, (C1-C6)alkyl, (C1-C6)alkoxy and trifluoromethyl;
- comprising reacting a compound of the formula
- with a dehydrating agent.
2 more elements
A process for preparing a compound of the formula
- wherein b is 0, 1, 2 or 3;
- Y is oxygen, sulfur, NH or N-acetyl;
- and each R3 is independently selected from the group consisting of halo, cyano, (C1-C6)alkyl, (C1-C6)alkoxy and trifluoromethyl;
- comprising
- (a) reacting a compound of the formula
- with hydroxyacetic acid, mercaptoacetic acid or 2-aminoacetic acid;
- (b) reacting a compound of formula IV so formed
- with a reducing agent and reacting the compound so formed with hydrochloric acid;
- (c) reacting a compound of formula III so formed
- with haloacetic acid in the presence of a base;
- and
- (d) reacting a compound of formula II so formed
- with a dehydrating agent.
10 more elements
A compound of the formula
A compound of the formula
A compound of the formula
Dependencies are inferred from the claim text.