1. Chemical properties of Tropisetron Hydrochloride
Tropisetron Hydrochloride is an alkaline, alkaline and hydrophobic colorless solid with a molecular weight of 389.00. It is soluble in various organic solvents such as dichloromethane, toluene and styrene, and slightly soluble in water.
2.Use of Tropisetron Hydrochloride
Tropisetron Hydrochloride is mainly used for the treatment of nausea and vomiting (PONV) after surgery and during radiotherapy for malignant tumors. It can also be used for more effective prevention and treatment of nausea and vomiting caused by other basic diseases (such as kidney disease and heart disease) as a follow-up compound drug treatment (including placebo).
3.Tropisetron hydrochloride is a 5-HT3 receptor antagonist, usually used to treat chemotherapy-induced nausea and vomiting. The following is a possible route to synthesize Tropisetron hydrochloride:
(1) Through the Michael addition reaction catalyzed by sodium hydroxide, 2-methyl-1H-indole-3-one and 4-phenyl-1,3-propanedione are reacted to produce 2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-one.
(2) Reaction of 2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-one with trichloroacetic acid to produce 3 - (2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-yl) propionic acid.
(3) 3 - (2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-yl) propionic acid is reacted with 2-chloroacetic acid to produce 3 - (2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-yl) propionic acid ethyl ester.
(4) Reaction of ethyl 3 - (2-methyl-4-phenyl-1,2,3,4-tetrahydroindole-3-yl) propionate with sodium trihydroxide to hydrolyze into Tropisetron.
(5) Finally, Tropisetron is reacted with hydrochloric acid to produce Tropisetron hydrochloride.
It should be noted that the above synthesis routes are for reference only, and there may be some changes and optimization in the actual synthesis process. In addition, chemical synthesis needs to be carried out under safe laboratory conditions and operated by experienced chemists.
4.Tropisetron Hydrochloride (TropHCl in English and Dolon hydrochloride in Chinese), with molecular formula C18H22ClNO3, is an indoxazole antipyretic, analgesic and antipsychotic drug. As a 5-hydroxytryptamine 3 receptor antagonist, its effective component is called "tropisetron", and its structure is developed based on the structure of oxazole-mediated fatty acid NCA, which is mainly used for anti-aversion reaction (fear of emotion), inhibition of nausea or vomiting, and treatment of open and closed randomized double-blind research reactions.
The discovery of Tropisetron can be traced back to the 1970s, when the British drug known as "Doron" was introduced by Janssen Pharmaceuticals Ltd for the treatment of patients with liver cirrhosis. The drug was first discovered by Janssen-Cilag Pharmaceutical Company in Germany, and then Dolon was also used to treat nausea and vomiting when cancer lymph node metastasis occurred.
With more and more studies on Dolong, more and more people have found that Dolong has anti-aversion, anti-nausea and anti-anxiety effects. According to many clinical studies, dolone can be used as an over-the-counter drug to resist aversion and has been found to have antidepressant effect, and is considered as an effective antidepressant.
In the 1990s, Dolon began to receive attention again and was developed as Tropisetron Hydrochloride or TropHcl. According to different diagnosis and treatment guidelines, it was regarded as an effective secondary or primary anti-anorexia drug, and also used as an antidepressant drug to relieve the obvious disorder of mood when depressed.
5.Users and annual exports of Tropisetron Hydrochloride
Tropisetron Hydrochloride is a relatively common drug, mainly used in Europe and the continent of the Americas, with the largest use in Europe. The main use countries are Germany, Switzerland, the United Kingdom, France, Israel and other countries. In 2016, the export volume of Europe and America reached 6027 kg, up 25.8% year on year.
6.Manufacturer of Tropesetron Hydrochloride
The main manufacturers of Tropisetron Hydrochloride include international companies such as Indiro, Geely, Iscon and Enito, and domestic companies such as Zhangzhou Dolphin and Hangzhou Dayuan. Among them, the company has obvious advantages in the production of such products, accounting for more than 60% of the export volume of European and American markets, and its export volume has been increasing since 2015.