MANUFACTURING METHOD OF BIFUNCTIONAL TETRAAZA MACROCYCLIC COMPOUNDS AND USE THEREOF

摘要

PURPOSE: A method for preparing bifunctional tetraaza microcyclic compound is provided to ensure high yield of the microcyclic compound without generation of cis-double substituted product. CONSTITUTION: A method for preparing a bifunctional tetraaza microcyclic compound comprises: a step of oxidizing a compound of chemical formula 1 to prepare a bisaminal compound of chemical formula 2; a step of alkylating the bisaminal compound to obtain protection group-conjugated trans compound of chemical formula 3; and a step of hydrolyzing the trans compound to obtain a compound of chemical formula 4. The bifunctional tetraaza microcyclic compound contains a compound of chemical formula 5 and pharmaceutically acceptable salt.