相似化合物
49773-20-8 146698-94-4 202197-68-0欧盟法规
REACH注册ECHA物质C&L通报上下游产品
CAS号49773-20-8 2-(甲磺酰基)乙胺 | CAS号49773-20-8 2-(甲磺酰基)乙胺 | CAS号388082-78-8 二甲苯磺酸拉帕替尼 | CAS号231277-92-2 拉帕替尼合成工艺路线路线简述
- 合成目标产物 2-Aminoethylmethylsulfone Hydrochloride 主要起始原料 2-(Methylthio)Ethylamine
- (文献来源)合成步骤主要原料 2-(Methylthio)Ethylamine
专利信息
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-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.
专利号:WO-2013080218-A1
优先权日:2011-11-28
标 题 :Novel intermediates and process for the preparation of lapatinib and its pharmaceutically acceptable salts
发明人:LAHIRI SASWATA; GUPTA NITIN; SINGH HEMANT KUMAR; HANDA VISHAL; SANGHANI SUNIL
权利人:FRESENIUS KABI ONCOLOGY LTD
摘要:The present invention discloses novel intermediates and processes for the synthesis of Lapatinib and its pharmaceutically acceptable salts thereof.
专利号:WO-2014170910-A1
优先权日:2013-04-04
标 题:Process for the preparation of lapatinib
发明人:MUDDASANI PULLA REDDY; TALASILA SAMBASIVA RAO; SATTI VENKATA REDDY; NEKKANTI SATISH CHOWDARY; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD
摘要:Present process relates to an improved and commercial process for the preparation of lapatinib of formula-I or its pharmaceutically acceptable p-toluenesulfonate salt involving novel intermediates of formulae-XVII, XVIII, and XIX. Present process utilizes Meerwein reaction as a key step in the aryl C-C bond formation step avoiding costly boronate coupling chemistry used in the conventional synthesis of lapatinib.
专利号:US-2025170267-A1
优先权日:2022-02-28
标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof
发明人:TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO
权利人:UBE CORP
摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).
专利号:WO-2014059956-A1
优先权日:2012-10-17
标题 :A method of producing the key intermediate of lapatinib synthesis
发明人:RADL STANISLAV; STEFKO MARTIN; CERNY JOSEF
权利人:ZENTIVA KS
摘要:The present invention relates to a production method of the compound of formula I, consisting in coupling the iodo derivative of formula III with boronic acid derivatives, catalyzed by suitable Pd catalysts in a solvent, wherein the boronic acid derivatives are cyclic boronates of the general formula VII, wherein R 1 , R 2 , R 3 and R 4 is H, or a C 1 -C 4 (un)branched alky and wherein X is either a bond or CR 5 R 6 wherein R 5 and R 6 is H, or a C 1 -C 4 (un)branched alkyl. Other aspects of the invention are cyclic boronates and use of the compound of formula I.