2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine intermediates
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United States of America Patent
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Apr 28, 1992
Issued Date -
N/A
app pub date -
Aug 13, 1991
filing date -
Dec 29, 1988
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Abstract
2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.
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