DERIVATIVES OF OPTICALLY ACTIVE N-SUBSTITUTED PYRROLIDINE, PIPERIDINE DERIVATIVE AND REAGENT FOR ASSAYING ACTIVITY OF BUTYRYL CHOLINE ESTERASE IN BRAIN CONTAINING THE SAME

摘要

PROBLEM TO BE SOLVED: To obtain the subject derivatives of optically active N-substituted pyrrolidine and piperidine capable of measuring activity of BchE not only in a brain after death but also in vivo targeting a living human or animal and from outside of a body in a noninvasive procedure.;SOLUTION: An optically active N-substituted pyrrolidine derivative of formulas I or II [R1 is a butyryl or valeryl group; R2 is (non)radioactive lower alkyl], e.g. (R)-N-methyl-3-butyryl-oxypyrrolidine. The derivative of formula I is obtained, for example, by reacting a derivative of formula III with butyl chloride (or valeryl chloride) in the presence of pyridine in a solvent such as methylene chloride, etc., at room temperature to obtain corresponding N-tert- butoxycarbonylbutyl (or valeryl) ester derivative, and then treating with HCl/ ethyl acetate, etc., at room temperature to give an amino ester derivative and then reacting with(non) radioactive methyl iodide. A reagent for assay of BchE activity is prepared by using the derivative of formula I or II as an active ingredient.;COPYRIGHT: (C)2001,JPO