CAS: 202917-18-8; Glucagon Receptor Antagonists-2
该化合物是一组化合物,旨在有选择地抑制 glucagon 受体,从而调节葡萄糖新陈代谢.这些对立体表现出对glucagon 受体的高度结合性和特殊性,使其具有研究代谢途径和潜在治疗应用的宝贵工具.主要优势包括:它们有能力抑制在2型糖尿病等条件下至关重要的肝糖生产.这些化合物的特点是其稳定性,选择性和在体外和活体模型中的可再生活动.其定义精细的药用动力学和药用动力学特征进一步支持了它们在临床前研究和药物开发中的使用.
- 英文名称Glucagon Receptor Antagonists-2
- 中文名称(αR,4S)-4-(4-氟-2-羟基苯基)-α-甲基-2,6-双(1-甲基乙基)-5-丙基-3-吡啶甲醇
- IUPAC名称5-fluoro-2-(3-((R)-1-hydroxyethyl)-2,6-diisopropyl-5-propylpyridin-4-yl)phenol
- 其它别名3-Pyridinemethanol, 4-(4-Fluoro-2-Hydroxyphenyl)-A-Methyl-2,6-Bis(1-Methylethyl)-5-Propyl-, (Ar,4S)-Rel- (9Ci); 3-Pyridinemethanol, 4-(4-Fluoro-2-Hydroxyphenyl)-α-Methyl-2,6-Bis(1-Methylethyl)-5-Propyl-, (αr,4S)-Rel- (9Ci); (Alphar,4S)-4-(4-Fluoro-2-Hydroxyphenyl)-Alpha-Methyl-2,6-Bis(1-Methylethyl)-5-Propyl-3-Pyridinemethanol; Glucagon Receptor Antagonists-2; 3-Pyridinemethanol, 4-(4-Fluoro-2-Hydroxyphenyl)-.Alpha.-Methyl-2,6-Bis(1-Methylethyl)-5-Propyl-, (.Alpha.R,4S)-Rel- (9Ci); Glucagon Receptor Antagonist 2; Glucagon Receptor Antagonists 2,Glucagon Receptor Antagonists2
- CAS编号202917-18-8
- MFCD编号:MFCD11616246
- 分子式:C22H30FNO2分子量:359.48
- 产品CID: 1030044
- 产品分类医药中间体 → 吡啶类化合物
物理性质
上下游产品
1-[4-(2-Benzyloxy-4-fluoro-phenyl)-2,6-diisopropyl-5-((E)-propenyl)-pyridin-3-yl]-ethanol 3-oxopentanedioic acid dimethyl ester dimethyl 2,6-diisopropyl-4-oxo-2H-pyran-3,5-dicarboxylate dimethyl 2,6-diisopropyl-4-methoxy-3,5-pyridine-dicarboxylate合成工艺路线路线简述
📜1,3-丙酮二羧酸二甲酯置于palladium On Activated Charcoal 吡啶,Lithium Aluminium Tetrahydride,氨,氢气,Potassium Carbonate,红铝,Pyridinium Chlorochromate体系中,用 四氢呋喃,甲醇,乙醚,乙醇,二氯甲烷,1,2-二氯乙烷,丙酮,甲苯 用作溶剂,化学反应 0.5H,反应生成(Alphar,4S)-4-(4-氟-2-羟基苯基)-Alpha-甲基-2,6-双(1-甲基乙基)-5-丙基-3-吡啶甲醇
参考文献:Integration Of Optimized Substituent Patterns To Produce Highly Potent 4-Aryl-Pyridine Glucagon Receptor Antagonists
标题:Integration Of Optimized Substituent Patterns To Produce Highly Potent 4-Aryl-Pyridine Glucagon Receptor Antagonists
摘要:Optimized Substituent Patterns In 4-Arul-Puridine Glucagon Receptor Antagonists Were Merged To Produce Highly Potent Derivatives Containing Both A 3-[(1R)-Hydroxyethyl] And A 2'-Hydroxy Group. Due To Restricted Rotation Of The Phenyl-Pyridine Bond,These Analogues Exist As Four Isomers. A Diastereoselective Methylcopper Reaction As Developed To Facilitate The Synthesis,And Single Isomers Ere Isolated With Activities In The Range Ic50 = 10 25 Nm. (C) 2002 Elsevier Science Ltd. All Rights Reserved.
Doi:10.1016/s0960-894X(02)00736-9
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2902600000-乙苯
2902700000-异丙基苯 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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主要参考文献
1. Ladouceur, G.H., Cook, J.H., Hertzog, D.L., et al. Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. Bioorg. Med. Chem. Lett. 12(23), 3421-3424 (2002).合成参考文献
参考文献:10.1016/s0960-894x(02)00736-9
摘要:Ladouceur GH, Cook JH, Hertzog DL, Jones JH, Hundertmark T, Korpusik M, Lease TG, Livingston JN, MacDougall ML, Osterhout MH, Phelan K, Romero RH, Schoen WR, Shao C, Smith RA. Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 2002 Dec;12(23):3421–4. doi: 10.1016/s0960-894x(02)00736-9.
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