- A 5 - chloro - 6 - (chloromethyl) uracil and its preparation method (by machine translation)
-
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)
- -
-
Paragraph 0043; 0044; 0045
(2017/08/28)
-
- Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides
-
Heterocycles adjacent to amides can have important influences on molecular conformation due to stereoelectronic effects exerted by the heteroatom. This was shown for imidazole- and thiazole-amides by comparing low energy conformations (ab initio MP2 and DFT calculations), charge distribution, dipole moments, and known crystal structures which support a general principle. Switching a heteroatom from nitrogen to sulfur altered the amide conformation, producing different three-dimensional electrostatic surfaces. Differences were attributed to different dipole and orbital alignments and spectacularly translated into opposing agonist vs antagonist functions in modulating a G-protein coupled receptor for inflammatory protein complement C3a on human macrophages. Influences of the heteroatom were confirmed by locking the amide conformation using fused bicyclic rings. These findings show that stereoelectronic effects of heterocycles modulate molecular conformation and can impart strikingly different biological properties.
- Reid, Robert C.,Yau, Mei-Kwan,Singh, Ranee,Lim, Junxian,Fairlie, David P.
-
supporting information
p. 11914 - 11917
(2014/10/16)
-
- Synthesis and in-vitro anti-hepatitis B virus activity of ethyl 6-Bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates
-
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.
- Chen, Dong,Liu, Yajing,Zhang, Shulan,Guo, Dexiang,Liu, Chunhong,Li, Sai,Gong, Ping
-
scheme or table
p. 158 - 164
(2011/10/05)
-
- Process For Preparing Chlorinated Carbonyl Compounds In Jet Loop Reactors
-
The present invention relates to a process for preparing chlorinated or partly chlorinated carbonyl compounds, which comprises reacting unchlorinated or partly chlorinated carbonyl compounds with a chlorinating agent in a jet loop reactor.
- -
-
Page/Page column 3-4
(2008/12/05)
-