METHODS FOR PREPARING MACROCYCLIC PRODUCTS BY RING-CLOSING DIINE METATHESIS

摘要

The invention relates to methods for preparing macrocyclic products with 9 ormore ring atoms by ring-closing diine metathesis of suitable diine substrates.The diine substrates can be converted into cycloakynes or into cycloalkadiinesby cyclodimerisation, depending on the particular reaction conditions. Anyalkyne metathesis catalyst can be used as the catalyst, regardless of whetherthey are heterogeneously or homogeneously present in the reaction medium. Thepreferred catalysts or pre-catalysts are transition metal alkylidinecomplexes, transition metal compounds which form alkylidine complexes underthe reaction conditions, and transition metal compounds with metalmetal triplebonds. The method can be carried out with numerous functional groups, solventsand additives. The macrocyclic cycloalkynes or cycloalkadiines formed can beconverted into numerous secondary products using known methods, especiallymacrocyclic cycloalkenes with a uniform configuration of the double bond, andused e.g. for synthesising epothilone or epothilone analogues.