CAS: 388082-77-7; N-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)-6-(5-(((2-(Methylsulfonyl)Ethyl)Amino)Methyl)Furan-2-yl)Quinazolin-4-Amine Bis(4-Methylbenzenesulfonate)

上下游产品

lapatanib toluene-4-sulfonic acid 2-(methylsulfonyl)ethylamine hydr°Chloride 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehydelapatinib monohydr°Chloride lapatinib hydrogen bromide salt lapatinib citric acid salt

拉帕替尼置于对甲苯磺酸体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 1.0H,以33%的收率获得产物二对甲苯磺酸拉帕替尼
参考文献:一种用于合成拉帕替尼或其中间体5-(4-羟基喹唑啉)-呋喃-2-甲醛的方法
标题:一种用于合成拉帕替尼或其中间体5-(4-羟基喹唑啉)-呋喃-2-甲醛的方法
摘要:本发明涉及一种用于合成拉帕替尼或其中间体5‑(4‑羟基喹唑啉)‑呋喃‑2‑甲醛的方法.合成所述中间体的方法包括所述方法包括如下步骤:在溶剂中在催化量的催化剂存在的情况下,使4‑羟基‑6‑硝基喹唑啉与水合肼反应,制得4‑羟基‑6‑氨基喹唑啉;在溶剂中在酸,亚硝酸钠和催化量的催化剂存在的情况下,使4‑羟基‑6‑氨基喹唑啉与呋喃甲醛反应,制得所述中间体.本发明还涉及一种合成拉帕替尼和/或其盐,拉帕替尼中间体和/或所述中间体的药学可接受的盐的方法,该方法使用所述中间体进行,并且该中间体由前述方法合成.本发明方法具有步骤简化,试剂便宜易得且利用率高,无重金属污染,反应条件/操作要求相对较低和/或产率高等优点.

专利信息

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-9359333-B2
优先权日:2013-01-14
标 题 :Efficient process for the preparation of Lapatinib and salts thereof by means of new intermediates
发明人：FONTANA FRANCESCO; PAIO ALFREDO
权利人:F I S —FABBRICA ITALIANA SINT S P A; F I S —FABBRICA ITALIANA SINT
摘要:The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. n In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-8853396-B2
优先权日:2011-03-25
标 题:Methods for the preparation of lapatinib and the salts thereof
发明人：FONTANA FRANCESCO
权利人:FONTANA FRANCESCO; ITALIANA SINT SPA
摘要:Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents.