CAS: 336113-53-2; (R)-N-(3-Aminopropyl)-N-(1-(3-Benzyl-7-Chloro-4-Oxo-3,4-Dihydroquinazolin-2-yl)-2-Methylpropyl)-4-Methylbenzamide

上下游产品

(R)-tert-butyl (3-((1-(3-benzyl-7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methylpropyl)amino)propyl)carbamate 4-methyl-benzoyl chloride 2-Amino-4-chlorobenzoic acid isopentanoyl chloride

📜3-苄基-2-(1-溴-2-甲基丙基)-7-氯喹唑啉-4-酮置于sodium Azide,三乙酰氧基硼氢化钠,氯化铵,N,N-二异丙基乙胺,O,O'-Dibenzoyl-L-Tartaric Acid,三氟乙酸,锌体系中,用 甲醇,二氯甲烷,乙酸乙酯,1,2-二氯乙烷,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 55.5H,反应生成 伊斯平斯
参考文献:Fluorinated Quinazolinones As Potential Radiotracers For Imaging Kinesin Spindle Protein Expression
标题:Fluorinated Quinazolinones As Potential Radiotracers For Imaging Kinesin Spindle Protein Expression
摘要:Anti-Mitotic Anti-Cancer Drugs Offer A Potential Platform For Developing New Radiotracers For Imaging Proliferation Markers Associated With The Mitosis-Phase Of The Cell-Cycle. One Interesting Target Is Kinesin Spindle Protein (Ksp)-An Atp-Dependent Motor Protein That Plays A Vital Role In Bipolar Spindle Formation. In This Work We Synthesised A Range Of New Fluorinated-Quinazolinone Compounds Based On The Structure Of The Clinical Candidate Ksp Inhibitor,Ispinesib,And Investigated Their Properties In Vitro As Potential Anti-Mitotic Agents Targeting Ksp Expression. Anti-Proliferation (Mtt And Brdu) Assays Combined With Additional Studies Including Fluorescence-Assisted Cell Sorting (Facs) Analysis Of Cell-Cycle Arrest Confirmed The Mechanism And Potency Of These Biphenyl Compounds In A Range Of Human Cancer Cell Lines. Additional Studies Using Confocal Fluorescence Microscopy Showed That These Compounds Induce M-Phase Arrest Via Monoaster Spindle Formation. Structural Studies Revealed That Compound 20-(R) Is The Most Potent Fluorinated-Quinazolinone Inhibitor Of Ksp And Represents A Suitable Lead Candidate For Further Studies On Designing F-18-Radiolabelled Agents For Positron-Emission Tomography (Pet). (C) 2012 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2012.11.013

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:JP-2005529076-A
优先权日:2002-02-15
标题:Synthesis of quinazolinone

专利号:US-8349899-B1
优先权日:2008-12-03
标题:Selective inhibitors of EG5 motors and methods of use
发明人：ARTERBURN JEFFREY; SHUSTER CHARLES
权利人:ARROWHEAD CT INC; ARTERBURN JEFFREY; SHUSTER CHARLES
摘要:Embodiments of the present invention comprises a compound of formula I or its enantiomer, diastereomer, stereoisomer or its pharmaceutically acceptable salt, methods of use and methods of synthesis.

专利号:US-7161002-B2
优先权日:2002-02-15
标 题 :Syntheses of quinazolinones
发明人：BERGNES GUSTAVE; HA EDWARD; YIANNIKOUROUS GEORGE; KALARITIS PANOS; YONCE BRANDON E; WELDAY JR KURT ALAN
权利人:SMITHKLINE BEECHAM CORP
摘要:The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: n nor a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.

专利号:US-9295731-B2
优先权日:2013-04-01
标题 :Cleavable drug conjugates, compositions thereof and methods of use
发明人：NGUYEN MARK QUANG
权利人:NGUYEN MARK QUANG
摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.