According to the present invention an enantiopure chelating compound of general Formula 10A or 10B is provided:wherein each of R1 through R3 is independently selected hydrogen, substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted C2-C20 alkenyl, substituted or unsubstituted C2-C20 alkynyl, substituted or unsubstituted C3-C10 cycloalkyl, substituted or unsubstituted C6-C60 aryl, or -Si(R4)(R5)(R6), and each of R4 through R6 is independently selected a substituted or unsubstituted group consisting of C1-C20 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, C1-C20 alkoxy, C3-C10 cycloalkyl, C6-C60 aryl, and C6-C60 aryloxy.The present invention further refers to a corresponding preparation method of the chelating compound and chelator coupled pharmaceuticals including the same.