首页|TYK2抑制剂BMS986202的合成工艺

TYK2抑制剂BMS986202的合成工艺

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BMS986202是一种有效的,具有选择性的口服活性TYK2 抑制剂,对包括JAK家族在内的激酶具有高度选择性,可用于IL-23 驱动的棘皮症、抗CD40 诱导的结肠炎和自发性狼疮的治疗,具有良好的开发和应用前景.以1-溴-2-甲氧基-3-硝基苯为起始原料,经还原、偶联、芳基化和酰胺化 4 步反应得到 BMS986202,并对BMS986202 的合成路线进行优化,总收率为85%,其结构经1H NMR和MS(ESI)表征.结果表明:该方法步骤简单,反应条件温和,操作方便,具有较好的工业化前景.
Synthesis Processs of TYK2 Inhibitor BMS986202
BMS986202,a potent,selective and orally active TYK2 inhibitor is remarkably selective o-ver other kinases including JAK family members and it can be used for the treatment of IL-23-driven acanthosis,anti-CD40-induced colitis,and spontaneous lupus,which has a good prospect of develop-ment and application.The improved synthetic route of BMS986202 has been developed.By using 1-bromo-2-methoxy-3-nitrobenzene as staring material,BMS986202 was obtained through four steps in-cluding reduction,coupling,arylation and amidation.The total yield was increased to 85%and the structure of product was characterized by 1H NMR and MS(ESI).The results showed that with the ad-vantages of mild reaction condition,simple step,convenient to handle,this route is suitable for the in-dustrial production.

BMS986202deucravacitinibsynthesisTYK2 inhibitorJAK inhibitorprocess im-provementSuzuki coupling reaction

张倩倩、李铭东、党诗涵、李春、李庶心、胡文祥、闵清

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湖北科技学院 药学院,湖北 咸宁 437100

江西中医药大学 药学院,江西 南昌 330000

苏州隆博泰药业有限公司,江苏 苏州 215000

北京神剑天军医学科学研究院京东祥鹄微波化学联合实验室,北京 101601

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BMS986202 氘可来昔替尼 合成 TYK2抑制剂 JAK抑制剂 工艺改进 Suzuki偶联反应

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(4)
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