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US 5,183,903 AGranted
Urea fusion process for the synthesis of 3-phenoxy-1-azetidinecarboxamides
AssigneeA. H. Robins Company, Incorporated
InventorsWilliam J. Welstead, Jr., Young S. Lo
Life of this patent
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Abstract
This invention relates to an improved process for the preparation of 3-phenoxy-1-azetidinecarboxamides of Formula I which are useful ##STR1## in the treatment of epileptic seizures. Under Formula I, n is 1 to 3, X is H, halogen, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acetyl, or aminocarbonyl, and R is H or methyl. This process involves heating a 3-phenoxyazetidine with urea to obtain the Formula I compound. Urea is inexpensive and easily removed by washing the solid Formula I product with water.
Claims11
A process for the preparation of compound having the formula:
- ##STR7## wherein n is 1 to 3, R is H or methyl, and X is hydrogen, halogen, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acetyl or aminocarbonyl and when n is 2 or 3, the values of X may be the same or different, which comprises heating together a compound having the formula:
- ##STR8## wherein n, X and R are as defined above, with from about 1 to about 10 molar equivalents of urea at from about 60.degree. C. to about 150.degree. C. for from 0.5 to 5 hours in the absence of a solvent.
Dependencies are inferred from the claim text.