CAS: 112733-06-9; 2-(3-(4-Bromo-2-Fluorobenzyl)-7-Chloro-2,4-Dioxo-3,4-Dihydroquinazolin-1(2H)-yl)Acetic Acid

该化合物是糖尿病和相关代谢紊乱,是一种化学化合物,主要研究其潜在的治疗用途,其功能是作为抗艾剂还原酶抑制剂,这意味着抑制导致将甘蔗糖转化成沙洛醇的酶,从而有可能减少与糖尿病有关的并发症,如...

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上下游产品

乙基[3-(4-溴-2-氟苄基)-7-氯-2,4-二氧代-3,4-二氢-1(2H)-喹唑啉基]乙酸酯 Ethyl 2-(3-(4-Bromo-2-Fluorobenzyl)-7-Chloro-3,4-Dihydro-2,4-Dioxo-1(2H)-Quinazolinyl)Acetate 112733-28-5
1,2,3,4-Tetrahydro-7-Chloro-2,4-Dioxoquinazolin-1-Ylacetic Acid 188293-91-6
7-氯-3,4-二氢-2,4-二氧代-1(2H)-喹唑啉乙酸乙基酯 Ethyl 2-(7-Chloro-3,4-Dihydro-2,4-Dioxo-1(2H)-Quinazolinyl)Acetate 112733-45-6

合成工艺路线路线简述

    📜2-氨基-4-氯苯甲酸置于盐酸,Potassium Carbonate,Sodium Hydroxide体系中,用 甲醇,水,N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 59.0H,反应生成折那司他
    参考文献:The Process Development Of A Novel Aldose Reductase Inhibitor,Fk366. Part 1. Improvement Of Discovery Process And New Syntheses Of 1-Substituted Quinazolinediones
    标题:The Process Development Of A Novel Aldose Reductase Inhibitor,Fk366. Part 1. Improvement Of Discovery Process And New Syntheses Of 1-Substituted Quinazolinediones
    摘要:This Contribution Describes Part 1 Of Process Development Of A Novel Aldose Reductase Inhibitor Fk366 (1). The Original Process Applied On A Laboratory Scale Was Improved From The Safety Viewpoint To Manufacture Materials On 500-L Scale Suitable For Toxicological And Pharmacological Evaluations. A New Process,Including Regioselective Alkylation Of Silylated Quinazolinedione,Provided A Practical And Cost-Effective Synthesis Of Fk366 In A Dramatically Increased Yield.
    Doi:10.1021/op0340661

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    专利信息


    专利号:US-9315483-B2
    优先权日:2007-09-13
    标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
    发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
    权利人:CONCERT PHARMACEUTICALS INC
    摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

    专利号:US-2025223262-A1
    优先权日:2022-03-31
    标 题 :Synthesis of morphinans with reduced herg activity and mop binding
    发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
    权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
    摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

    专利号:EP-1551403-B1
    优先权日:2002-10-10
    标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia
    发明人:SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN
    权利人:ARENA PHARM INC
    摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.

    专利号:US-2006122240-A1
    优先权日:2002-11-05
    标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof
    发明人:SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y
    权利人:ARENA PHARM INC
    摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

    专利号:US-2007032537-A1
    优先权日:2003-06-13
    标题:5-Substituted 2h-pyrazole-3-carboxylic acid derivatives as agonists for the acid receptor rup25 for the treatment of dyslipidemia and related diseases
    发明人:SEMPLE GRAEME; GHARBAOUI TAWFIK; SHIN YOUNG-JUN; DECAIRE MARC; AVERBUJ CLAUDIA L; SKINNER PHILIP J
    权利人:ARENA PHARM INC
    摘要:The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like the substituents are defined in claim 1.

    专利号:WO-2009035652-A1
    优先权日:2007-09-13
    标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

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    主要参考文献


    1: Zenarestat. FK 366, FR 74366, FR 901366. Drugs R D. 2002;3(4):235-7. Review. Erratum in: Neurology 2001 Apr 24;56(8):1124. Epub 2002 Mar 22. doi: 10.1016/j.brainres.2008.10.018. Epub 2008 Nov 1. Natural progression of diabetic peripheral neuropathy in the Zenarestat study population. Diabetes Care. 2004 May;27(5):1153-9.

    合成参考文献


    参考文献:10.1007/s11892-005-0048-6
    摘要:Mojaddidi M, Quattrini C, Tavakoli M, Malik RA. Recent developments in the assessment of efficacy in clinical trials of diabetic neuropathy. Curr Diab Rep. 2005 Dec;5(6):417–22. doi: 10.1007/s11892-005-0048-6.
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