5-溴-2-甲基苯胺置于tetrafluoroboric Acid,18-冠醚-6,Potassium Acetate,Potassium Hydroxide,Sodium Nitrite体系中,用 甲醇,氯仿,水 作为反应溶剂,化学反应 5.0H,反应生成 6-溴-1-甲基吲唑 参考文献:Aza Spiro Alkane Derivatives As Inhibitors Of Metallproteases 标题:Aza Spiro Alkane Derivatives As Inhibitors Of Metallproteases
专利信息
专利号:US-12258318-B2 优先权日:2019-06-17 标题 :Synthesis method for 1-methyl-1H-indazole-6-carboxylic acid 发明人:YANG JUN; Xue Duoqing; WU YONG; CHEN LIHUANG; ZHAI LIANHUA 权利人:ACCELA CHEMBIO CO LTD 摘要:The present application provides a synthesis method for 1-methyl-1H-indazole-6-carboxylic acid. The synthesis method comprises: using 2-fluoro-4-bromobenzaldehyde and methylhydrazine as raw materials to obtain 6-bromo-1-methylindazole by means of an annulation reaction, and then performing a methyl formate reaction and a hydrolysis reaction, so as to obtain the 1-methyl-1H-indazole-6-carboxylic acid. The synthesis method provided in the present application can directly synthesize a 1-position methyl substituted indazole without isomers, thereby avoiding the problem that impurities are difficult to be removed in subsequent separation, thus improving the purity of a product. The yield of the annulation reaction can reach 85%.
专利号:US-2012077802-A1 优先权日:2009-06-10 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-9051289-B2 优先权日:2013-09-26 标 题 :Process and intermediates for preparing GPR40 agonists 发明人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN 权利人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I n nwherein R S denotes F or CF 3 , R a denotes H or C 1-4 -alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.