Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于copper(II) Sulfate,Sodium Bromide体系中,化学反应生成 2-溴-5-甲基噻唑 参考文献:The Preparation Of Thiazole Grignard Reagents And Thiazolyllithium Compounds1,2 标题:The Preparation Of Thiazole Grignard Reagents And Thiazolyllithium Compounds1,2 摘要: DOI:10.1021/ja01144A031
专利信息
专利号:US-8772301-B2 优先权日:2009-12-18 标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof 发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D 权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:WO-2024131948-A1 优先权日:2022-12-22 标题 :Method for preparing p2x3 inhibitor 发明人:ZHANG XUEJUN; ZANG YANG; LI QUN; ZHANG BO; LI YUAN; YANG QIONGFENG; XIA QINGFENG; YUE YANG; YANG JUN; LI LIE 权利人:HUMANWELL HEALTHCARE GROUP CO LTD; WUHAN HUMANWELL INNOVATIVE DRUG RES AND DEVELOPMENT CENTER LIMITED COMPANY 摘要:The present invention belongs to the field of drug synthesis. Specifically, disclosed is a method for preparing a P2X3 inhibitor, i.e., 2-fluoro-5-(((2S,3R)-3-hydroxybutan-2-yl)oxy)-3(5-methylthiazol-2-yl)-N-((R)-1-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)benzamide (I-1). The method comprises the following steps: using 3-bromo-2-fluoro-5-iodobenzoic acid as a starting material, substituting iodine with a hydroxyl group and subjecting a carboxyl group to methyl esterification to obtain a compound 1C; subjecting the compound 1C and B2(pin)2 to a coupling reaction to obtain 1D; subjecting the compound 1D and 2-bromo-5-methylthiazole to a coupling reaction to obtain 1E; substituting the compound 1E with 1F to then obtain a compound 1H; hydrolyzing 1H under the action of a base to obtain 1I, and subjecting the compound 1I and 1L to a condensation reaction to obtain a product I-1. The synthesis route provided by the present invention makes it easy to control product quality, has a high yield and is suitable for industrial production.
参考文献:10.1021/acsmedchemlett.2c00429 摘要:Proj M, Hrast M, Knez D, Bozovičar K, Grabrijan K, Meden A, Gobec S, Frlan R. Fragment-Sized Thiazoles in Fragment-Based Drug Discovery Campaigns: Friend or Foe ACS Med. Chem. Lett. 2022 Nov 03;13(12):1905–10. doi: 10.1021/acsmedchemlett.2c00429.