2 results about "Tropisetron" patented technology

This invention relates to the pharmaceutical field, specifically disclosing the synthesis of a tromethamine linker and its application in drug coupling. The three-load linker uses tromethamine as the parent core, with three hydroxyl groups of tromethamine binding to three loads, and an amino group linked to maleimide, thus constructing a three-load linker. The linker proposed in this invention allows the three loads to be linked to three effector molecules through click chemistry, cyclization reactions, or disulfide bonds; the maleimide is then linked to a targeting ligand to construct a drug coupling agent with three load effector molecules.

This invention belongs to the field of deuterated labeled compound synthesis technology, and discloses a method for deuterating indole compounds and its application. The deuteration method of this invention includes the following steps: mixing an indole compound, a transition metal catalyst, a complex ligand, an additive, and a deuteration solvent, reacting to obtain a deuterated product; the complex ligand includes a first ligand and a second ligand; the first ligand includes a lactam compound; the second ligand includes a pyridone compound; and the deuteration solvent includes deuterated acetic acid. The deuteration method of this invention achieves highly selective hydrogen-deuterium exchange at multiple sites on the indole ring of indole compounds (especially the difficult-to-modify C4-C7 sites) through the synergistic effect of the catalyst, the dual ligand, and the deuteration solvent system. Furthermore, it can be applied to the deuteration synthesis of drugs such as the anti-inflammatory drug indomethacin, the cancer adjuvant therapy drug tropisetron, and the neuromodulator melatonin, providing key technical support for the development of deuterated drugs.