CAS: 231278-20-9; N-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)-6-Iodoquinazolin-4-Amine

上下游产品

CAS号98556-31-1 4-氯-6-碘喹唑啉 | CAS号202197-26-0 3-氯-4-(3-氟苄氧基)苯胺 | CAS号1227853-05-5 N(1)-(3-chloro-... | CAS号132131-24-9 2-氨基-5-碘苯腈 | CAS号202197-25-9 4-(3-Fluoro-ben... | CAS号443882-99-3 3-氯-4-(3-氟苄氧基)硝基苯 | CAS号944483-37-8 3-chloro-4-(3-f... | CAS号619-08-9 2-氯-4-硝基酚 | CAS号456-41-7 3-氟苄溴 | CAS号388082-78-8 二甲苯磺酸拉帕替尼 | CAS号231278-84-5 5-[4-[[3-氯-4-[(... | CAS号231277-92-2 拉帕替尼 | CAS号388082-81-3 GW 583340二盐酸盐

6-碘-4(H)-喹唑啉酮置于氯化亚砜,N,N-二甲基甲酰胺体系中,用 异丙醇 用作溶剂,化学反应 2.0H,反应生成4-[3-氯-4-(3-氟苄基氧)苯基氨基]-6-碘喹唑啉
参考文献:具有异羟肟酸部分的新型6-(1,2,3-三唑-4-基)-4-氨基喹唑啉衍生物的合成和研究,用于癌症治疗.
标题:具有异羟肟酸部分的新型6-(1,2,3-三唑-4-基)-4-氨基喹唑啉衍生物的合成和研究,用于癌症治疗.
摘要:通过将egfr / Her2和hdac抑制剂的关键药效团合并为一个化合物,合成了一系列新的egfr,Her-2和hdac多靶点抑制剂.化合物9A-1含有4-苯胺基喹唑啉和c-6三唑连接的异羟肟酸长烷基链,对这些酶表现出优异的抑制作用(化合物9D对野生型egfr,Hdac1和hdac6表现出最佳的抑制效能,Ic50值分别为0.12 Nm,0.72Nm和3.2Nm).此外,化合物9B和9D有效抑制了五种人类癌细胞系的增殖(ic50值在0.49至8.76μm之间).进一步的机理研究表明,化合物9D在细胞水平上还调节egfr和her2的磷酸化以及组蛋白h3的超乙酰化,并诱导bt-474细胞显着的凋亡.所以,
Doi:10.1016/j.Bmc.2016.10.006

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:WO-2024185814-A1
优先权日:2023-03-06
标题:Method for producing aryl compound containing tritylsulfanyl group
发明人：OKAZOE TAKASHI; NOZAKI KYOKO; GATZENMEIER Tim; LIU YUE
权利人:AGC INC; UNIV TOKYO
摘要:The present invention provides: a substrate for achieving the highly efficient synthesis of an aryl compound containing a tritylsulfanyl group; a method for producing a compound containing an SF 5 group using the substrate; and others. The present invention is a method for producing an aryl compound containing a tritylsulfanyl group, the method comprising thiotritylating a halogenated aryl compound represented by general formula (1) [wherein A 1 represents an aryl group that may have a substituent or a heteroaryl group that may have a substituent; and X represents a halogen atom] using [(triphenylmethyl)sulfanyl]potassium or [(triphenylmethyl)sulfanyl]sodium to produce an aryl compound containing a tritylsulfanyl group, the aryl compound being represented by general formula (2) [wherein A 1 is the same as A 1 in general formula (1); and Ph represents a phenyl group].

专利号:CN-108484541-B
优先权日:2018-04-11
标 题 :Synthesis method of 5-formyl furan-2-ethyl nitrobenzoate