1,2,4-三唑并[3,4- a ]吡啶和相关的杂环以及取代的三嗪是在各种药物和农用化学试剂中普遍发现的支架。在这里,我们报告了一种高效且实用的方法,该方法使用DMF及其衍生物进行[4 + 1]和[5 + 1]环化反应,以制备这些杂环。这种无金属的反应利用了贮存稳定的DMF作为溶剂和碳供体,使用咪唑氯化物作为催化剂的优势,温和的反应条件可耐受广泛的底物范围并替代。制备的3-未取代的1,2,4-三唑并[3,4- a ]吡啶和衍生物允许在3-位进一步引入各种官能团。
The Base-Promoted Annulation of 2-Hydrazinyl Pyridine and CO<sub>2</sub>
toward Triazolones
作者:Xiaopeng Wu、Song Sun、Bingbing Wang、Jiang Cheng
DOI:10.1002/adsc.201700869
日期:2017.11.10
A base‐promoted annulation of 2‐hydrazinyl pyridine and atmospheric pressure of CO2 has been developed in the presence of silane as reducing reagent, affording a series of triazolones in moderate to excellent yields. CO2 served as a carbonyl source in this transfomation. Moreover, benzamidrazones also worked well under this procedure. Thus, it represents a green, sustainable and straightforward pathway
[EN] SLC2A TRANSPORTER INHIBITORS<br/>[FR] INHIBITEURS DU TRANSPORTEUR SLC2A
申请人:IOMET PHARMA LTD
公开号:WO2014187922A1
公开(公告)日:2014-11-27
Provided is a SLC2A class I transporter inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein A and Z may be the same or different and are each independently selected from C, N, O and S; each X may be the same or different and is independently selected from C, N, O and S; R1 and R5 may be present or absent and may be the same or different and are each selected from H and a substituted or unsubstituted organic group; Z completes a ring with each X, each ring comprising from 3 to 8 ring atoms including the X, A, and Z, each ring atom being independently selected from C, N, O and S, and each ring atom being unsubstituted or independently substituted with H or a substituted or unsubstituted organic group; and wherein the bonds between all of the atoms in the rings including the X, A, and Z may independently be single bonds or double bonds, provided that when X or a ring atom is O or S the bonds to X are single bonds.
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.