CAS: 1369764-02-2; (1R,2S)-2-(((2,4-Dimethylpyrimidin-5-yl)Oxy)Methyl)-2-(3-Fluorophenyl)-N-(5-Fluoropyridin-2-yl)Cyclopropanecarboxamide

上下游产品

17H16ClFN2O2C17H16ClFN2O2 2-amino-5-fluoropyridine (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)cyclopropanecarboxylic acid (1S,2R)-1-(3-fluorophenyl)-2-(hydroxymethyl)cyclopropane-1-carboxylic acid(1R,2S)-2-(((2-methyl-4-bromomethylpyrimidin-5-yl)oxy)methyl)-N-(5-fluoropyridin-2-yl)-2-(3-fluorophenyl)cyclopropanecarboxamide (1R,2S)-2-(((2-methyl-4-hydroxymethylpyrimidin-5-yl)oxy)-methyl)-N-(5-fluoropyridin-2-yl)-2-(3-fluorophenyl)-cyclopropanecarboxamide (1R,2S)-2-{[(4-fluoromethyl-2-methylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide

[(1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)Oxy]Methyl}-2-(3-Fluorophenyl)Cyclopropyl]Methyl Acetate置于sodium Chlorite,Sodium Dihydrogenphosphate,2-甲基-2-丁烯,草酰氯,二甲基亚砜,N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate,Sodium Hydroxide体系中,用 乙醇,二氯甲烷,水,N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 4.5H,反应生成莱博雷生
参考文献:(1 R,2 S)-2-{[((2,4-二甲基嘧啶-5-基)氧基]甲基}-2-(3-氟苯基)-N-(5-氟吡啶-2-基)环丙烷甲酰胺的发现(e2006):高效有效的口服orexin受体拮抗剂
标题:(1 R,2 S)-2-{[((2,4-二甲基嘧啶-5-基)氧基]甲基}-2-(3-氟苯基)-N-(5-氟吡啶-2-基)环丙烷甲酰胺的发现(e2006):高效有效的口服orexin受体拮抗剂
摘要:Orexin / Hypocretin受体是g蛋白偶联受体的一个家族,由orexin-1(ox 1)和orexin-2(ox 2)受体亚型组成.食欲素受体在整个中枢神经系统中表达,并参与睡眠/觉醒周期的调节.由于这些受体的调节构成了与睡眠和清醒控制相关的疾病(如失眠)的新型治疗的有希望的靶标,因此,Orexin受体拮抗剂的开发已成为药物发现研究中的重要重点.在这里,我们报告了新型orexin受体拮抗剂的设计,合成,表征和结构-活性关系(sar).对先前开发的化合物的核心结构进行了各种修改(-)-5(铅分子)产生具有改进的化学和药理学特征的化合物.研究提供了潜在的治疗剂,(1 R,2 S)-2-{[((2,4-二甲基嘧啶-5-基)氧基]甲基}-2-(3-氟苯基)-N-(5-氟吡啶)-2-基)环丙烷甲酰胺(e2006),一种口服活性,有效的食欲素拮抗剂.通过使用睡眠参数测量,在体内研究中在小鼠中证明了该功效.
Doi:10.1021/acs.Jmedchem.5B00217

专利信息

专利号:US-11891375-B2
优先权日:2021-07-26
标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates
发明人：AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

专利号:US-9828336-B2
优先权日:2012-02-17
标题:Methods and compounds useful in the synthesis of orexin-2 receptor antagonists
发明人：MONIZ GEORGE ANTHONY; WILCOXEN ANNIE ZHU; BENAYOUD FARID; TANAKA TOSHIAKI; SORIMACHI KEIICHI
权利人:EISAI R&D MAN CO LTD
摘要:The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

专利号:US-2023092143-A1
优先权日:2021-07-26
标 题:Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of lemborexant using the intermediates

专利号:ES-2933074-B2
优先权日:2021-07-26
标 题 :SYNTHESIS PROCEDURE OF 2,4-DIMETHYLPYRIMIDIN-5-OL, NEW INTERMEDIATE OF SUCH PROCEDURE AND USE OF THE PRODUCT IN THE SYNTHESIS OF LEMBOREXANT

专利号:JP-2023017733-A
优先权日:2021-07-26
标 题:Method for synthesizing 2,4-dimethylpyrimidine-5-ol, novel intermediate for the method, and use of product in synthesis of lemborexant

专利号:CN-104114524-B
优先权日:2012-02-17
标 题 :Methods and compounds for the synthesis of orexin-2 receptor antagonists