Process for the preparation of 7-azabicyclo[4.1.0]hept-3-ene-3-carboxylic acid esters

摘要

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<2 >from the azabicyclohept-3-ene (VI)