CAS: 571190-30-2; 6-Acetyl-8-Cyclopentyl-5-Methyl-2-((5-(Piperazin-1-yl)Pyridin-2-yl)Amino)Pyrido[2,3-D]Pyrimidin-7(8H)-One

上下游产品

CAS号827022-32-2 盐酸帕博西尼

6-Acetyl-8-Cyclopentyl-5-Methyl-2-[[5-(1-Piperazinyl)-2-Pyridinyl]Amino]-5,6-Dihydropyrido[2,3-D]Pyrimidyl-7(8H)-One置于tetrahydropyridine Dichromate Nickel (II),溶剂黄146体系中,化学反应 8.0H,以95.3%的收率获得产物帕布昔利布
参考文献:一种帕博西尼的制备方法
标题:一种帕博西尼的制备方法
摘要:本发明属于医药化工领域,具体涉及一种帕博西尼的制备方法,超声‑微波辅助合成法将2‑乙酰基‑2‑丁烯酸甲酯,丙二腈和胍类化合物ⅲ三组分一并反应,快速,高产率的得到化合物ⅳ;然后在亚硝酸钠和次磷酸发生去氨基还原反应反应生成化合物ⅴ;再与卤代环戊烷在催化剂作用下发生偶联反应反应生成化合物ⅵ;最后在催化剂tpnd的作用下发生脱氢反应制得帕博西尼.本发明具有反应条件温和,工艺流程简单合理,反应时间短,后处理简单,产品质量高,产率高等优点.

专利信息

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人：ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:WO-2024199465-A1
优先权日:2023-03-30
标 题:Unnatural amino acid in cellulo synthesis for site-specific protein modification
发明人：CHAN MICHAEL KENNETH; LEE MARIANNE; CHENG JIAHUI
权利人:UNIV HONG KONG CHINESE
摘要:Provided are genetically modified host cells containing engineered enzymes that support the synthesis of unnatural amino acids, such as D-Cys-ε-Lys, and the incorporation of such unnatural amino acids into a newly synthesized protein. These cells are therefore capable of in vivo or in cellulo synthesis of a protein containing one or more unnatural amino acids strategically placed at pre-determined locations for site-specific modification of the protein. Also provided are the corresponding methods for in vivo synthesis of modified proteins as well as the modified proteins produced by the method.

专利号:US-2023002411-A1
优先权日:2019-12-20
标 题:Deuterated analogues of selenophenochromenes, synthesis thereof, and methods of using same agents
发明人：ARSENJANS PAVELS
权利人:LATVIAN INST ORGANIC SYNTHESIS
摘要:The present invention relates to a novel cancer curing deuterated selenopheno [h] chromene derivatives, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of cancer by administration of such substances.