Process for the preparation of 7-azabicyclo[4.1.0]hept-3-ene-3-carboxylic acid esters
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United States of America Patent
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Sep 14, 2004
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N/A
app pub date -
Aug 13, 2002
filing date -
Nov 2, 1999
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Expired
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Abstract
The present invention provides a method of producing 7-azabicyclo[4.1.0]hept-3-ene-3-carboxylic acid ester (VII) economically, industrially advantageously and efficiently in a large amount. The present invention relates to a production method of compound (VII), which includes reacting epoxide (I) with amine (II) to give aminodiol (III), reacting the aminodiol (III) with a sulfonylating agent in the presence of a base to give azabicyclohept-2-ene (IV), reacting the azabicyclohept-2-ene (IV) with alcohol (V) in the presence of a Lewis acid to give azabicyclohept-3-ene (VI), and eliminating the 7-position substituent R.sup.2 from the azabicyclohept-3-ene (VI) ##STR1##
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