CAS: 16064-08-7; 6-Iodoquinazolin-4-One

相似化合物

202197-77-1 491-36-1 16353-27-8

上下游产品

CAS号5326-47-6 2-氨基-5-碘苯甲酸 | CAS号149-73-5 原甲酸三甲酯 | CAS号32658-67-6 2-氨基-5-碘苯甲酰胺 | CAS号77287-34-4 甲亚胺酸 | CAS号77317-55-6 5-碘代邻氨基苯甲酸甲酯 | CAS号122-51-0 原甲酸三乙酯 | CAS号64392-62-7 formamidinium a... | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号383432-38-0 2-甲氧基-N-[(2E)-3... | CAS号388082-78-8 二甲苯磺酸拉帕替尼 | CAS号201298-40-0 6-碘-3-甲基-3H-喹唑啉-4-酮 | CAS号98556-31-1 4-氯-6-碘喹唑啉 | CAS号231278-84-5 5-[4-[[3-氯-4-[(... | CAS号231278-20-9 N-[3-氯-4-(3-氟苄氧... | CAS号537705-05-8 6-碘-N-(3-甲基-4-(...

2-氨基-5-碘苯甲酸 以 Formamide 用作溶剂,化学反应 12.0H,以92.6%的收率获得6-碘-4(H)-喹唑啉酮
参考文献:一种拉帕替尼的制备方法
标题:一种拉帕替尼的制备方法
摘要:本发明公开了一种拉帕替尼的制备方法,尤其是本发明的合成方法中利用起始原料2‑氨基‑5‑碘苯甲酸与环合试剂制得中间体6‑碘‑3,4‑二氢喹唑啉‑4‑酮(ⅲ),该中间体6‑碘‑3,4‑二氢喹唑啉‑4‑酮(ⅲ)在硫代试剂,卤代甲烷条件下生成喹唑啉硫醚(ⅴ),再进一步合成目标分子.该反应使得终产品拉帕替尼收率提高,避免了不稳定中间体4‑氯代喹唑啉产物的生成,同时也避免了具有腐蚀性三氯化磷,五氯化磷,二氯亚砜,光气或三氯氧磷等氯化剂的使用,适合工业化生产.

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-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-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: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: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