Ethyl cinnamate: care for the cradle of life, radical gynecological tumors

According to the latest statistics from the health department, the incidence of cervical cancer, ovarian cancer, and breast cancer has risen significantly in recent years, and has become the three major killers of urban women, and shows a trend of youthfulness. In order to care for the cradle of the lives of the ovaries and breasts, to treat ovarian cancer and breast cancer, and to find good therapeutic drugs, medical pharmacy experts have conducted long-term and arduous studies. Experts found that paclitaxel has a very good effect on the treatment of ovarian and breast cancer.

Paclitaxel is a complex secondary metabolite in the genus Taxus, and is the only drug known to promote microtubule polymerization and stabilize the polymerized microtubules. Isotope tracing showed that paclitaxel binds only to the polymerized microtubules and does not react with unpolymerized tubulin dimers. When cells contact paclitaxel, they accumulate a large number of microtubules in the cell. The accumulation of these microtubules interferes with various functions of the cell, in particular, the cell division stops at the mitosis and blocks the normal cell division. Through II-III clinical studies, paclitaxel is mainly applicable to ovarian cancer and breast cancer, and it also has a certain effect on lung cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma, and brain tumor. However, the production of paclitaxel is extremely low. At present, the world needs about 4 tons per year, but the output is only about 1 ton. In particular, docetaxel, which is more active than paclitaxel, can only be produced through industrial synthesis and its yield is extremely low. One of the main factors that leads to the low price of taxol is that the catalyst for synthesis of this drug cannot be recycled.

Recently, experts from the Department of Pharmacy of China's Fourth Military Medical University, after intense study, invented a recyclable and reusable chiral catalyst. In its role, the ethyl ester of cinnamic acid is used as the raw material, through the key steps of asymmetric dihydroxylation reaction and the seven steps of esterification, cyclization, ring opening, catalytic reduction and group protection to synthesize the paclitaxel C13 fragment or polyene Paclitaxel fragments were then coupled with bakatins to synthesize the anticancer drug paclitaxel or docetaxel.

Currently, synthetic taxol and docetaxel at home and abroad are generally synthesized using asymmetric catalytic reactions or chiral sources. However, due to the high cost of chiral catalysts used or the long reaction steps, production costs are high and they cannot be put into industrial production. Recyclable and reusable chiral catalysts, suitable for industrial production, significantly reduce production costs and can greatly increase production.

Experts said that the invention of the chiral catalyst, and the use of ethyl cinnamate, will be able to take good care of the cradle of life, cure gynecological tumors and benefit women!

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