To provide a method for selectively and efficiently producing a fluorocycolopropane derivative suitable as a production intermediate for a compound useful for production of a medicine, etc., by directly introducing fluorine atom to the cyclopropane skeleton.
The objective fluorocyclopropane derivative of formula III (R2 is H or a lower alkyl) is produced by reacting (A) a compound of the formula CH2=CH-CO-OR2 (R1 is a lower alkyl) with (B) a compound of the formula ArSOCH2X (Ar is an aryl; X is Cl or Br) to provide (C) a compound of formula I, reacting the component C with (D) molecular fluorine to provide (E) a compound of formula H, reductively desulfonylating the component E and, if necessary, hydrating the desulfonylated compound. Moreover, the reduction is preferably performed by using a sodium amalgam, and a step for treating the trans- form compound of a byproduct with a base to change the one into the component E is preferably included.
TOYODA AKEMI
HAYAKAWA ISAO
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