5-(2,4-Diamino-Pyrimidin-5-Yloxy)-4-Isopropyl-2-Methoxy-Benzenesulfonyl Chloride置于氨,盐酸,水体系中,用 环丁砜,甲醇,乙醇,水 用作溶剂,化学反应 18.0H,反应生成Af-219或mk-7264 参考文献:Process For Synthesis Of Phenoxy Diaminopyrimidine Derivatives 标题:Process For Synthesis Of Phenoxy Diaminopyrimidine Derivatives 摘要:一种制备化合物的方法,其化学式为kor或其盐或溶剂合物,其中r1如本文所定义,该方法包括处理化合物的方法,其化学式为jor或其盐或溶剂合物,使用氨来形成化合物的方法.
专利信息
专利号:US-11584724-B2 优先权日:2018-04-23 标 题:Process for synthesis of a phenoxy diaminopyrimidine compound 发明人:MALONEY KEVIN M; BASU KALLOL; DI MASO MICHAEL JAMES; HUMPHREY GUY R; LEE ALFRED Y; PENG FENG; REN HONG; ZHANG SIWEI 权利人:MERCK SHARP & DOHME; WERTHENSTEIN BIOPHARMA GMBH; MERCK SHARP & DOHME LLC 摘要:Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
专利号:US-9643934-B2 优先权日:2006-10-04 标 题:Process for synthesis of phenoxy diaminopyrimidine derivatives 发明人:DVORAK CHARLES ALOIS; GREEN KEENA LYNN; LEE GARY R 权利人:ROCHE PALO ALTO LLC 摘要:A method for preparing a compound of formula k n n n n n n n n n n n n or a salt or solvate thereof,n wherein R 1 is as defined herein, n n the method comprising treating a compound of formula j n n n n n n n n n n n n n n n n or a salt or solvate thereof, n with ammonia, to form the compound of formula k.
专利号:MX-2020011258-A 优先权日:2018-04-23 标题:NOVEL PROCESS FOR SYNTHESIS OF A COMPOUND OF PHENOXY DIAMINOPYRIMIDINE.
专利号:BR-112020020549-A2 优先权日:2018-04-23 标 题 :NEW PROCESS FOR THE SYNTHESIS OF A DIAMINOPYRIMIDINE PHENOXY COMPOUND
专利号:US-8580960-B2 优先权日:2006-10-04 标题:Process for synthesis of phenoxy diaminopyrimidine derivatives
专利号:US-2008086004-A1 优先权日:2006-10-04 标题 :Process for synthesis of phenoxy diaminopyrimidine derivatives
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合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 参考文献:10.1097/mib.0000000000000047 摘要:Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for Developing Purinergic Drugs for Gastrointestinal Diseases. Inflammatory Bowel Diseases. 2014 Jul;20(7):1259–87. doi: 10.1097/mib.0000000000000047.