CAS: 341-24-2; 7-Fluoro-1H-Indazole

📜2,3-二氟苯乙酮置于一水合肼体系中,用41%的收率获得产物7-氟-1H-吲唑
参考文献:Fluorinated Analogues Of Marsanidine,A Highly α2-Ar/imidazoline I1 Binding Site-Selective Hypotensive Agent. Synthesis And Biological Activities
标题:Fluorinated Analogues Of Marsanidine,A Highly α2-Ar/imidazoline I1 Binding Site-Selective Hypotensive Agent. Synthesis And Biological Activities
摘要:The Aim Of These Studies Was To Establish The Influence Of Fluorination Of The Indazole Ring On The Pharmacological Properties Of Two Selective Alpha(2)-Aradrenoceptor (Alpha(2)-Ar) Agonists: 1-[(Imidazolidin-2-yl) Imino]-1H-Indazole (Marsanidine,A) And Its Methylene Analogue 1-[(4,5-Dihydro-1H-Imidazol-2-yl) Methyl]-1H-Indazole (B). Introduction Of Fluorine Into The Indazole Ring Of A And B Reduced Both Binding Affinity And Alpha(2)-Ar/i-1 Imidazoline Binding Site Selectivity. The Most Alpha(2)-Ar-Selective Ligands Were 6-Fluoro-1-[(Imidazolidin-2-yl)Imino]-1H-Indazole (6C) And 7-Fluoro-1-[(Imidazolidin-2-yl)Imino]-1H-Indazole (6D). The In Vivo Cardiovascular Properties Of Fluorinated Derivatives Of A And B Revealed That In Both Cases The C-7 Fluorination Leads To Compounds With The Highest Hypotensive And Bradycardic Activities. The Alpha(2)-Ar Partial Agonist 6C Was Prepared As A Potential Lead Compound For Development Of A Radiotracer For Pet Imaging Of Brain Alpha(2)-Ars. (C) 2014 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2014.09.083

专利信息

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: