Methods for preparing functional tetraazacycloalkane compounds using a specific cyclic bisaminal compound  (WO2013072491)

This patent allows to elaborate a large variety of C-functionalized tetraazamacrocyles from the protected oxocyclam (A). TETA (E), TE2A (F) and CB-TE2A (G) derivatives are obtained from the protected cyclam intermediate (B). The protected oxocyclam (A) is conveniently used to generate mono N-functionalized cyclams (C) and cross-bridged cyclams (D), which offer the possibility to access dissymmetric TETA (H) or CB-TE2A (I).


Related publications:
J. Org. Chem. 2014, 79, 1885−1899 (DOI: 10.1021/jo4028566)
Org. Biomol. Chem. 2015, 13, 11302–11314 (DOI: 10.1039/c5ob01618e)
RSC Advances 2015, 5, 85898−85910 (DOI: 10.1039/C5RA17133D)

technology disclosed in the WO2013072491 patent
technology disclosed in the WO2015071334 patent


Picolinate cross-bridged cyclams, chelates with metallic cations and use thereof (WO2015071334)

This patent describes the synthesis and use of cross-bridged cyclams with picolinate arms bearing at least one coupling function in R1, R2, R3, R4 or R5 positions.


Related publication:
Inorg. Chem. 2014, 53, 5269−5279 (DOI: 10.1021/ic500491c)