Urea fusion process for the synthesis of 3-phenoxy-1-azetidineca

Details Urea fusion process for the synthesis of 3-phenoxy-1-azetidineca Urea fusion process for the synthesis of 3-phenoxy-1-azetidineca

1991-11-26

1993-02-02

Brust, Joseph Paul

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548953, C07D20504

Patent

active

051839032

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.

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Davis and Underwood, J. Amer. Chem. Soc. 44, 2595-2604 (1922) The Urea Dearrangement.
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