CAS: 1097917-15-1; N2-(2-(Isopropylsulfonyl)Phenyl)-N4-(2-Methoxy-4-(4-(4-Methylpiperazin-1-yl)Piperidin-1-yl)Phenyl)-1,3,5-Triazine-2,4-Diamine

上下游产品

1-methyl-piperazine 1-[3-methoxy-4-({4-[2-(propane-2-sulfonyl)anilino]-1,3,5-triazin-2-yl}amino)phenyl]piperidin-4-one 1-(1-(3-methoxy-4-nitrophenyl)piperidin-4-yl)-4-methylpiperazine 4-chloro-N-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazin-2-amine2-[(4-{[2-(isopropylsulfonyl)phenyl]amino}-1,3,5-triazin-2-yl)amino]-5-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenol

📜6-Chloro-N2-{2-Methoxy-4-[4-(4-Methylpiperazin-1-yl)Piperidin-1-Yl]Phenyl}-N4-[2-(Propane-2-Sulfonyl)Phenyl]-1,3,5-Triazine-2,4-Diamine置于palladium 10% On Activated Carbon,氢气,甲酸铵体系中,用 甲醇 用作溶剂,50.0 °C,100.0 Kpa 条件下,反应 3.0H,以29.6 Mg的收率获得asp 3026; N2-[2-甲氧基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-N4-[2-[(1-甲基乙基)磺酰基]苯基]-1,3,5-三嗪-2,4-二胺
参考文献:有效和选择性的间变性淋巴瘤激酶(alk)抑制剂asp3026的改进的生产路线和多态控制.
标题:有效和选择性的间变性淋巴瘤激酶(alk)抑制剂asp3026的改进的生产路线和多态控制.
摘要:描述了我们为改进间变性淋巴瘤激酶(alk)抑制剂asp3026(1)所做出的努力.由于起始原料从2,4-二氯-1,3,5-三嗪(6)变为氰尿酰氯(9)的后期转化,从而实现了1的经济高效且实用的合成.中间体酮13的还原胺化反应生成高反应性的n-甲基哌嗪部分.经过改进的工艺避免了原始合成方法带来的挑战,并为数百公斤的高质量api提供了高经济效率,可操作性和可重复性.此外,还讨论了第二代合成途径中多晶型控制的研究顺序,以获得热力学上期望的,最稳定的多晶型形式a04.
Doi:10.1021/acs.Oprd.8B00427

专利信息

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.