次黄嘌呤置于对甲苯磺酸,三氯氧磷体系中,用 四氢呋喃,N,N-二甲基乙酰胺 作为反应溶剂,化学反应 2.0H,反应生成 6-氯-9-(四氢-2-吡喃基)嘌呤 参考文献:Synthesis And Full Characterisation Of 6-Chloro-2-Iodopurine,A Template For The Functionalisation Of Purines 标题:Synthesis And Full Characterisation Of 6-Chloro-2-Iodopurine,A Template For The Functionalisation Of Purines 摘要:从次黄嘌呤中简单高效地合成了 6-氯-2-碘嘌呤.这一策略依赖于使用哈氏碱和三丁基氯化锡对 6-氯-9-(四氢吡喃-2-基)嘌呤进行区域特异性石化/淬火.对产物和中间产物的 Hmbc NMR 研究证实了这种方法的区域选择性.通过单晶 X 射线衍射测定了最终二卤代嘌呤及其 9 保护前体的分子结构. DOI:10.1039/b312629C
专利号:US-9732097-B2 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor 发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI 权利人:INCYTE CORP 摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
专利号:US-2016362426-A1 优先权日:2015-05-11 标题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor
专利号:US-9567337-B2 优先权日:2013-12-20 标题 :Process methods for phosphatidylinositol 3-kinase inhibitors 发明人:BREMNER STACY; EVARTS JERRY; SUJINO KEIKO; TRAN DUONG; VIZITIU DRAGOS 权利人:GILEAD CALISTOGA LLC 摘要:A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.
专利号:US-7176312-B2 优先权日:2001-10-12 标 题:Kinase inhibitor scaffolds and methods for their preparation 发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S 权利人:IRM LLC 摘要:General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
专利号:WO-2016183060-A1 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor
专利号:US-5164390-A 优先权日:1988-03-03 标 题:6-substituted purinyl piperazine derivatives 发明人:HAJOS ZOLTAN G; KANOJIA RAMESH M; PRESS JEFFERY B 权利人:ORTHO PHARMA CORP 摘要:6-substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.
摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 353. 摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 359.