5 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 relates to the field of pharmaceutical synthesis, specifically a method for synthesizing tropisetron. Compared with traditional methods, the tropisetron synthesis method provided by this invention offers a more efficient, faster, more environmentally friendly, milder, and more selective synthetic route. Based on the action of the Pd single-atom catalyst, it exhibits excellent selectivity for indole, an N-H substrate, enabling the synthesis of N-H substituted tropisetron. This solves the problem that existing technologies can only synthesize N-CH3 substituted tropisetron analogs using 1-methylindole, an N-CH3 substrate, as a starting material. The yield of tropisetron synthesized by this invention is close to 98%, and the product can be purified to meet the purity standards of the Chinese Pharmacopoeia through a simple purification process, facilitating large-scale industrial production. By optimizing the coordination structure of the Pd single-atom catalyst and maintaining the positive valence state of Pd, this invention can directly activate the C-H bond at the 3-position of indole without the need for external I2 and K2CO3, and produces no waste residue after the reaction.

The invention relates to the field of medicine synthesis, in particular to a synthesis method of tropisetron. Compared with the traditional method, the synthesis method of tropisetron provided by the invention has the advantages that the synthesis route is more efficient, rapid, environment-friendly and mild, and the selectivity is higher. On the basis of the effect of the Pd monatomic catalyst, the Pd monatomic catalyst has good selectivity on indole serving as an N-H substrate, tropisetron with a substituent group being N-H can be synthesized, and the problem that in the prior art, an N-CH3 substituted tropisetron analogue can only be synthesized by taking 1-methylindole serving as an N-CH3 substrate as a raw material is solved. The yield of the synthesized tropisetron is close to 98%, the purity of the product can reach the medication standard of Chinese pharmacopoeia through a simple purification process, and large-scale industrial production is facilitated. The coordination structure of the Pd monatomic catalyst is optimized, the positive valence state of Pd is kept, a C-H bond at the 3-position of indole can be directly activated, I2 and K2CO3 do not need to be additionally added, and no waste residues are generated after the reaction.

The invention relates to a tropisetron mesylate composition tablet, which is prepared from the following components: tropisetron mesylate, POCl3, NaBH4, N, N '-carbonyl diimidazole, methoxy polyethylene glycol amine, 4-dimethylaminopyridine, corn starch, cane sugar, lactose, sodium carboxymethyl cellulose and magnesium stearate. The invention also relates to a preparation process of the tropisetron mesylate composition tablet. The preparation method comprises the following steps: mixing tropisetron mesylate with an ethanol solution to obtain tropisetron free alkali, formylating by using POCl3, reducing by using NaBH4 to introduce an active hydroxyl group, and reacting by using N, N-dimethylformamide to obtain the tropisetron mesylate. The compound is further activated by N, N '-carbonyldiimidazole and is coupled with methoxy polyethylene glycol amine through catalysis of 4-dimethylaminopyridine, so that the water solubility can be improved, and the purpose of increasing the dissolution rate to improve the action effect of the medicine is achieved.

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.