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参考文献: A Method Of Producing The Key Intermediate Of Lapatinib Synthesis[fr] Procédé De Production De L'Intermédiaire Clé Pour La Synthèse De Lapatinib
标题: A Method Of Producing The Key Intermediate Of Lapatinib Synthesis[fr] Procédé De Production De L'Intermédiaire Clé Pour La Synthèse De Lapatinib
摘要:本发明涉及一种化合物i的生产方法,包括将化合物iii的碘衍生物与硼酸衍生物偶联,在溶剂中由适当的pd催化剂催化,其中硼酸衍生物为一般式vii的环硼酸酯,其中r1,R2,R3和r4为h,或者为c1-C4(非)支链烷基,其中x为键或cr5R6,其中r5和r6为h,或者为c1-C4(非)支链烷基.该发明的其他方面包括环硼酸酯和化合物i的用途.

专利信息

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: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.

专利号:CN-106632287-B
优先权日:2016-12-19
标 题 :The Isatine derivatives and its application in preparation of anti-tumor drugs of isatin heterozygosis quinazoline compounds synthesis