CAS: 1257213-50-5; (R)-1-(4'-(3-Methyl-4-(((1-Phenylethoxy)Carbonyl)Amino)Isoxazol-5-yl)-[1,1'-Biphenyl]-4-yl)Cyclopropane-1-Carboxylic Acid

上下游产品

1-{4'-[3-Methyl-4-((R)-1-Phenyl-Ethoxycarbonylamino)-Isoxazol-5-Yl]-Biphenyl-4-Yl}-Cyclopropanecarboxylic Acid Ethyl Ester 1380650-63-4
1-{4'-[3-Methyl-4-((R)-1-Phenyl-Ethoxycarbonylamino)-Isoxazol-5-Yl]-Biphenyl-4-Yl}-Cyclopropanecarboxylic Acid Isopropyl Ester 1380650-70-3
[5-(4-溴苯基)-3-甲基异恶唑-4-基]氨基甲酸(R)-1-苯基乙基酯 (R)-1-Phenylethyl (5-(4-Bromophenyl)-3-Methylisoxazol-4-yl)Carbamate 1228690-37-6
Benzyl 5-(4'-(1-(Ethoxycarbonyl)Cyclopropyl)Biphenyl-4-yl)-3-Methylisoxazole-4-Carboxylate 1380650-62-3
5-(4'-(1-(Ethoxycarbonyl)Cyclopropyl)-[1,1'-Biphenyl]-4-yl)-3-Methylisoxazole-4-Carboxylic Acid 1257214-10-0
5-(4'-(1-(Isopropoxycarbonyl)Cyclopropyl)Biphenyl-4-yl)-3-Methylisoxazole-4-Carboxylic Acid 1380650-69-0
Methyl 5-(4'-(1-(Isopropoxycarbonyl)Cyclopropyl)Biphenyl-4-yl)-3-Methylisoxazole-4-Carboxylate 1380650-68-9

📜(R)-(+)-1-苯基乙醇置于四羟基二硼,二氯双[二叔丁基-(4-二甲基氨基苯基)膦]钯(II),叠氮磷酸二苯酯,N,N-二异丙基乙胺体系中,用 2-甲基四氢呋喃,甲醇 用作溶剂,化学反应 18.0H,反应生成-[3-甲基-4-[[[((R)-1-苯基乙基)氧基]羰基]氨基]异恶唑-5-基]联苯-4-基]环丙烷羧酸
参考文献:通过串联硼基化-铃木法开发lpa-1拮抗剂bms-986020的简明多千克合成方法
标题:通过串联硼基化-铃木法开发lpa-1拮抗剂bms-986020的简明多千克合成方法
摘要:描述了通过钯催化的串联硼酸化/ Suzuki反应合成bms-986020(1)的方法.在四步中,使用四羟基二硼进行有效的硼酸酯化步骤,然后进行串联的铃木反应,使用有效的钯化催化剂进行条件评估.该方法论解决了早期合成路线的缺点,并最终用于活性药物成分1的多公斤级合成.对该硼化反应的进一步评估显示出与一系列取代的芳基溴化物和碘化物作为偶联伙伴的有用的反应性.这些发现代表了一种实用,有效,温和且可扩展的硼酸化方法.
Doi:10.1021/acs.Oprd.7B00301

专利信息

专利号:US-11739065-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:WO-2022162606-A1
优先权日:2021-01-30
标 题:Heterocyclic compounds as kinase inhibitor and uses thereof
发明人：YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK
权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD
摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)