DOTMA-based amides (DOTMAMs) as a platform for the development of PARACEST MRI contrast agents

作者：Suchy M; Li A X; Milne M; Bartha R; Hudson R H E^*

来源：RSC Advances, 2016, 6(67): 62647-62655.

DOI：10.1039/c6ra11741d

A synthetic methodology leading to previously unknown DOTMA-based secondary amides (DOTMAMs) has been developed. Alkylation of cyclen with L-lactic acid-derived pseudohalides was used as a key step affording the alkyl-and aryl-decorated DOTMAMs. Amino acid-decorated DOTMAMs were obtained via peptide coupling between DOTMA and protected amino acids. Metallation of the DOTMAMs ligand with Tm3+ gave complexes exhibiting proximal amide proton based paramagnetic CEST effects at < -50 ppm relative to water.

• 出版日期2016