CAS: 959122-11-3; (1R,2R)-2-(4'-(3-Phenylureido)-[1,1'-Biphenyl]-4-Carbonyl)Cyclopentanecarboxylic Acid

该化合物是一个复杂的有机化合物,其特征是其多功能组和立体化学.它有一个环球环,有助于其三维结构,并包含多种碳基组,增强其反应性和形成氢基的潜力.一个苯基氨基组的存在表明它与生物目标的潜在相互作用,使其对药用化学感兴趣.具体的立体化学学(1R2R)表明,由于它的空间安排,它可能表现出独特的生物活动或药用基因特性.该化合物可能因其潜在的治疗应用,特别是药物设计,其脂度和水量的平衡以及与特定生物受体的相互作用能力对于功效至关重要.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

CAS号959122-10-2 Methyl (1R,2R)-... | CAS号819056-67-2 N-苯基-N'-[4-(4,4... | CAS号791594-13-3 (1R,2R)-2-(4-溴苯... | CAS号1214270-80-0 2-bromo-6-(4-br... | CAS号108-94-1 环己酮 | CAS号1655-07-8 2-环己酮甲酸乙酯 | CAS号586-75-4 4-溴苯甲酰氯 | CAS号103-71-9 异氰酸苯酯 | CAS号214360-73-3 4-氨基苯硼酸频哪醇酯

合成工艺路线路线简述

  • 733740-98-2 = 959122-11-3 [标题:Reaction Conditions
    标题:Catalysis With Diboron(4)/pyridine: Application To The Broad-Scope [3 + 2] Cycloaddition Of Cyclopropanes And Alkenes
    作者:Ding,Zhengwei; Liu,Zhi; Wang,Zhijun; Yu,Tao; Xu,Ming; Et Al
    参考文献:Journal Of The American Chemical Society 日期:2022 卷标:144(19) 页码:8870-8882]

    959122-10-2 = 959122-11-3
    反应条件:1.1 Reagents: Lithium Hydroxide Solvents: Tetrahydrofuran,Water; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; < Ph 7
    标题:Preparation Of Ureidobiphenyls As Inhibitors Of Diacylglycerol O-Acyltransferase Type 1 (Dgat-1).
    参考文献:World Intellectual Property Organization]

    791594-13-3 + 819056-67-2 = 959122-11-3
    反应条件:1.1 Reagents: Dipotassium Phosphate Catalysts: (Sp-4-2)-[1,1′-Bis[bis(1,1-Dimethylethyl)Phosphino-Kp]Ferrocene]Dichloropalladiu... Solvents: Ethanol,Dimethylformamide,Water; 24 H,20 °C
    标题:Process Development Of A Diacyl Glycerolacyltransferase-1 Inhibitor
    作者:Ravn,Matthew M.; Wagaw,Seble H.; Engstrom,Kenneth M.; Mei,Jianzhang; Kotecki,Brian; Et Al
    参考文献:Organic Process Research & Development 日期:2010 卷标:14(2) 页码:417-424]

    959122-10-2 = 959122-11-3
    反应条件:1.1 Reagents: Lithium Hydroxide Solvents: Tetrahydrofuran,Water; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 7,Rt
    标题:Validation Of Diacyl Glycerolacyltransferase I As A Novel Target For The Treatment Of Obesity And Dyslipidemia Using A Potent And Selective Small Molecule Inhibitor
    作者:Zhao,Gang; Souers,Andrew J.; Voorbach,Martin; Falls,H. Doug; Droz,Brian; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2008 卷标:51(3) 页码:380-383]

    959122-10-2 = 959122-11-3
    反应条件:1.1 Reagents: Lithium Hydroxide Solvents: Tetrahydrofuran,Water; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; < Ph 7
    标题:Cycloalkanecarboxylic Acid Derivatives As Inhibitors Of Diacylglycerol O-Acyltransferase Type 1 Enzyme And Their Preparation,Pharmaceutical Compositions And Use In The Treatment Of Diseases
    参考文献:World Intellectual Property Organization
📜2-环己酮甲酸乙酯置于aluminum (Iii) Chloride,Dipotassium Hydrogenphosphate,氯化亚砜,Dichloro[1,1'-Bis(Di-T-Butylphosphino)Ferrocene]Palladium(II),(S)-(-)-N-甲基-1-苯基乙胺,溴,Sodium Hydroxide体系中,用 乙醇,氯仿,醋酸异丙酯,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 25.0H,反应生成 (1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸
参考文献:Process Development Of A Diacyl Glycerolacyltransferase-1 Inhibitor
标题:Process Development Of A Diacyl Glycerolacyltransferase-1 Inhibitor
摘要:A Synthesis Of A Selective Diacyl Glycerolacyltransferase-1 (Dgat-1) Inhibitor,1,Is Described. The Synthesis Illustrates A Diketone Favorskii Reaction On 9 In Place Of The More Common Ketoester Variant For Generation Of The Dicarboxycyclopentane Core,The Development Of An Efficient Classical Resolution Of A Key Cyclopentyl Ketoacid Intermediate 4,And An Ambient Temperature Suzuki-Miyaura Coupling Which Avoids Epimerization Of The Labile Aryl Ketone Of 1.
DOI:10.1021/op900310V

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专利信息


专利号:US-12016933-B2
优先权日:2020-11-25
标题:Method for stimulating axonal regeneration
发明人：YANG CHAO; WANG XU; LIU KAI
权利人:UNIV HONG KONG SCIENCE & TECH
摘要:A method of promoting axonal regeneration can include directing neuronal lipid synthesis away from triglyceride synthesis and toward phospholipid synthesis. The method can include administering to the patient a therapeutically effective amount of an inhibitor compound selected from the group consisting of a Lipin-1 inhibitor, a diglyceride acyltransferase inhibitor, and combinations thereof or administering a gene editing therapy to the patient that reduces expression of LIPIN1 or a diglyceride acyltransferase gene.

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主要参考文献


1: Tsuda N, Kumadaki S, Higashi C, Ozawa M, Shinozaki M, Kato Y, Hoshida K, Kikuchi S, Nakano Y, Ogawa Y, Furusako S. Intestine-targeted DGAT1 inhibition improves obesity and insulin resistance without skin aberrations in mice. PLoS One. 2014 Nov 18;9(11):e112027. doi: 10.1371/journal.pone.0112027.
2: King AJ, Segreti JA, Larson KJ, Souers AJ, Kym PR, Reilly RM, Zhao G, Mittelstadt SW, Cox BF. Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31. doi: 10.1124/jpet.109.154047. Epub 2009 May 28. 637(1-3):155-61. doi: 10.1016/j.ejphar.2010.03.056. Epub 2010 Apr 10. 33(4):271-278. doi: 10.1080/15376516.2022.2124898. Epub 2022 Sep 28.

合成参考文献


参考文献:10.1016/j.bmcl.2011.07.109
摘要:Motiwala H, Kandre S, Birar V, Kadam KS, Rodge A, Jadhav RD, Mahesh Kumar Reddy M, Brahma MK, Deshmukh NJ, Dixit A, Doshi L, Gupte A, Gangopadhyay AK, Vishwakarma RA, Srinivasan S, Sharma M, Nemmani KVS, Sharma R. Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 2011 Oct;21(19):5812–7. doi: 10.1016/j.bmcl.2011.07.109.
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