Synthetic process of decitabine

Abstract

The invention relates to a method for preparing Decitabine. The particular proposal for solving the technical problem is as follows: 2-deoxidtion-D-ribose, 10 percent of HCL methanol solution, methoxyacetic acetic anhydride, HMDS, acetic anhydride, tri-silicyl tri-fluorine methane sulfonic acid ester, acetic acid amine, etc. are adopted as raw materials to synthesize the Decitabine; the target product of the Decitabine is obtained through the five steps of reactions, namely, methylation, acylation, trimethyl silication, ammoniation and deacylation with a total yield of above 18.4 percent and a product purity of above 99.7 percent.

Description

technical field [0001] The invention relates to a synthetic method of chemical medicine, in particular to a synthetic method of decitabine. Background technique [0002] Decitabine, its drug name: Decitabine; registered name: Decitabine; drug alias: 5-azaCd, Azadc; trade name: Dacogen; chemical name: 4-amino-1-(2-deoxy-β-D-erythro Ribofuranose)-1,3,5-triazin-2(1H)-one. [0003] Decitabine is a 2'-deoxycytidine analogue developed by SuperGen Corporation of the United States, which can be converted into a 5'-monophosphate deoxycytidine analogue in vivo, and incorporated into DNA under the action of DNA polymerase to inhibit DNA synthesis And methylation, leading to cell differentiation or apoptosis, thereby inhibiting the growth of tumor cells, it can not inhibit DNA synthesis in vitro, but can cause hypomethylation in tumor cells, and maintain the related cell differentiation and proliferation control of genes function, and is currently undergoing clinical trials in refract...

AI Technical Summary

Problems solved by technology

1-(3,5-di-D-acetyl-2-deoxy-D-ribose)-5-azacytosine is passed through ammonia gas at room temperature in methanol, and the product is recrystallized with methanol after hydrolysis, but the reaction The final step is treated with ammonia gas, which is not easy to control during the experiment

Images