CAS: 98556-31-1; 4-Chloro-6-Iodoquinazoline

上下游产品

6-碘-4(H)-喹唑啉酮 6-Iodoquinazolin-4(3H)-One 16064-08-7

2-氨基-5-碘苯甲酸甲酯置于草酰氯体系中,用 四氢呋喃,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.0H,反应生成 4-氯-6-碘喹唑啉
参考文献:상피세포성장인자수용체 변이체를 가진 종양 진단 및 종양 성장 억제 활성을 갖는 신규 화합물 및 이를 포함하는 의학적 용도
标题:상피세포성장인자수용체 변이체를 가진 종양 진단 및 종양 성장 억제 활성을 갖는 신규 화합물 및 이를 포함하는 의학적 용도
摘要:本发明涉及一种具有上皮细胞生长因子受体突变体的肿瘤诊断和抑制肿瘤生长活性的新化合物或其盐,包括其作为造影剂的使用,以及包含其作为有效成分的egfr相关癌症治疗或预防药物组合物.根据本发明,新化合物或其盐可以选择性地抑制egfr突变体,而不抑制野生型egfr,因此可以治疗和预防egfr相关癌症,如肺癌,结肠癌或乳腺癌,特别是有效地治疗和预防非小细胞肺癌,而伊莫替尼和塔塞帕钠无效的肺癌.此外,根据本发明,新化合物或其盐可以针对具有egfr T790M突变的癌细胞或对zd1839敏感性的癌细胞进行选择性响应,而不是野生型egfr过度表达的癌细胞,因此可以作为可用于清晰区分egfr相关癌细胞的造影剂.

专利信息

专利号:US-7825244-B2
优先权日:2005-06-10
标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
发明人：BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.

专利号:US-2005192298-A1
优先权日:2004-02-27
标 题 :Crystal forms of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide
发明人：LI ZHENG J; LEONARD JASON A
权利人:PFIZER
摘要:Crystal forms of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide. A crystal form is useful in the synthesis of salts and complexes of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide. A crystal form also improves stability of tabletted or capsuled E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide as a drug product.

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-2007021436-A1
优先权日:2005-06-10
标 题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis

专利号:CA-2611219-A1
优先权日:2005-06-10
标题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis