CAS: 945966-46-1; N-(4-(4-Fluorophenyl)-2,2-Dimethyl-3-Oxo-3,4-Dihydro-2H-Benzo[b][1,4]Oxazin-7-yl)Methanesulfonamide

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上下游产品

7-Amino-4-(4-Fluorophenyl)-2,2-Dimethyl-2H-1,4-Benzoxazin-3(4H)-One 945968-84-3
7-氨基-2,2-二甲基-2H-苯并[b][1,4]恶嗪-3(4H)-酮 7-Amino-2,2-Dimethyl-2H-Benzo[b][1,4]Oxazin-3(4H)-One 105807-83-8
2,2-二甲基-7-硝基-2H-苯并[b][1,4]噁嗪-3(4H)-酮 2,2-Dimethyl-7-Nitro-2H-Benzo[b][1,4]Oxazin-3(4H)-One 85160-83-4

合成工艺路线路线简述

  • 1560020-87-2 = 945966-46-1
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Dimethyl Sulfoxide,Water; 25 °C; Overnight,25 °C1.2 Reagents: Hydrochloric Acid Solvents: Dimethyl Sulfoxide,Water; 25 °C; 5 H,25 °C
    标题:Method For Producing 1,4-Benzoxazine Compound
    参考文献:World Intellectual Property Organization]

    945968-84-3 = 945966-46-1
    反应条件:1.1 Reagents: Pyridine Solvents: Chloroform; Cooled; 18 H,Rt
    标题:Preparation Of Benzoxazine Derivatives And Analogs As Regulators Of Mineralocorticoid Receptor For Treatment Of Hypertension,Heart Failure,Myocardial Infarction,Etc.
    参考文献:Japan]

    945968-84-3 = 945966-46-1
    反应条件:1.1 Reagents: Pyridine Solvents: Chloroform; Cooled; 18 H,Rt1.2 Reagents: Sodium Bicarbonate Solvents: Water; Rt
    标题:Preparation Of Benzoxazines And Related Nitrogen-Containing Heterobicyclic Compounds As Mineralocorticoid Receptor Modulators.
    参考文献:World Intellectual Property Organization
📜N-[4-(4-Fluorophenyl)-2,2-Dimethyl-3-Oxo-3,4-Dihydro-2H-1,4-Benzoxazin-7-Yl]-N-(Methylsulfonyl)Methanesulfonamide 以86的收率获得产物阿帕利酮
参考文献:Method For Producing 1,4-Benzoxazine Compound
标题:Method For Producing 1,4-Benzoxazine Compound
摘要:本发明提供了一种在避免安全和健康风险的情况下生产用作药物的1,4-苯并噁嗪化合物的工业优势方法.具体而言,本发明提供了一种生产1,4-苯并噁嗪化合物[a]的方法,该方法包括以下方案中的三个步骤,即将化合物[a]中7位的氨基转化为二甲基磺酰氨基,将化合物[b]与硼酸化合物偶联,以及将化合物[c]中的7位转化为单甲基磺酰氨基.在上述方案中,Ms为甲磺酰基,R'和r''分别为氢原子等.

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✅ COA系统入驻 | 共享模式

主要参考文献


1: Kintscher U, Bakris GL, Kolkhof P. Novel non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease. Br J Pharmacol. 2022 Jul;179(13):3220-3234. doi: 10.1111/bph.15747. Epub 2022 Jan 13.
13:896947. doi: 10.3389/fphar.2022.896947.
3: Patel V, Joharapurkar A, Jain M. Role of mineralocorticoid receptor antagonists in kidney diseases. Drug Dev Res. 2021 May;82(3):341-363. doi: 10.1002/ddr.21760. Epub 2020 Nov 12. 25(2):120-130. doi: 10.1007/s10157-020-01963-z. Epub 2020 Sep 24.

合成参考文献


参考文献:10.1002/cpdd.855
摘要:Nakamura T, Kawaguchi A. Phase 1 Studies to Define the Safety, Tolerability, and Pharmacokinetic and Pharmacodynamic Profiles of the Nonsteroidal Mineralocorticoid Receptor Antagonist Apararenone in Healthy Volunteers. Clin Pharmacol Drug Dev. 2021 Apr;10(4):353–65.
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