CAS: 898280-07-4; N4-(5-Cyclopropyl-1H-Pyrazol-3-yl)-N2-((3-Isopropylisoxazol-5-yl)Methyl)-6-(4-Methylpiperazin-1-yl)Pyrimidine-2,4-Diamine

N-(4,6-Dichloropyrimidin-2-yl)-N-(Prop-2-Ynyl)Acetamide置于potassium Hydrogencarbonate体系中,用 N,N-二甲基乙酰胺,醋酸异丙酯 作为反应溶剂,化学反应 39.5H,反应生成 N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺
参考文献:Process Development And Multikilogram Syntheses Of Xl228 Utilizing A Regioselective Isoxazole Formation And A Selective Snar Reaction To A Pyrimidine Core
标题:Process Development And Multikilogram Syntheses Of Xl228 Utilizing A Regioselective Isoxazole Formation And A Selective Snar Reaction To A Pyrimidine Core
摘要:Route Scouting,Process Development,And Multikilogram Syntheses Of An Igf-1R/src/bcr-Abl Inihibitor Are Reported. Key Aspects Of The Developed Route Are A Regioselective [3 + 2] Isoxazole Formation On A Pyrimidine Core And A Selective Snar Addition Of An Aryl Amine To A Symmetrical Dichloro Substituted Pyrimidine. The Route Contains Six Synthetic Steps And Was Demonstrated Twice On Scale,Delivering 4.6 And 11.2 Kg (25% And 16% Overall Yield),For Phase I Clinical Studies.
DOI:10.1021/op400137M

专利信息

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.