88-00-6Relevant articles and documents
A 5 - chloro - 6 - (chloromethyl) uracil and its preparation method (by machine translation)
-
Paragraph 0043; 0044; 0045, (2017/08/28)
The present invention provides a 5 - chloro - 6 - (chloromethyl) uracil and its preparation method, comprises the following steps: (1), in order to-acetyl-acetic acid ethyl ester as the raw material, obtained by chlorination of the reaction process for preparing 4 - chloro acetyl ethyl acetate, 4 - chloro acetyl ethyl acetate through the chlorination reaction, to obtain 2, 4 - dichloro acetyl ethyl acetate; (2), the step (1) in the 2, 4 - dichloro-acetyl-acetic acid ethyl ester with urea in an acidic solvent, under the heating condition obtained by the reaction of 5 - chloro - 6 - (chloromethyl) uracil. The method has the raw materials are easy, simple operation, the method is reliable, low cost, and is suitable for industrial production and the like. The preparation of 5 - chloro - 6 - (chloromethyl) pyrimidine has the advantages of high purity in the urine, the purity is greater than 96%, can reach 99.4%. (by machine translation)
Synthesis and in-vitro anti-hepatitis B virus activity of ethyl 6-Bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates
Chen, Dong,Liu, Yajing,Zhang, Shulan,Guo, Dexiang,Liu, Chunhong,Li, Sai,Gong, Ping
scheme or table, p. 158 - 164 (2011/10/05)
A series of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylate derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in HepG2.2.15 cells. Nearly half of the tested compounds were proved to be highly effective in inhibiting the replication of HBV DNA with IC50 values ranging from 1.3 to 9.1 μM. Among them, 10o and 10s were identified as the most promising compounds.