合成目标产物 2-Chloro-5-Cyanopyridine 主要起始原料 2-(6-Chloropyridin-3-yl)Acetic Acid And Urea
14906-64-0 = 33252-28-7 + 6602-54-6 + 89284-61-7 反应条件:1.1 Reagents: Phosphorus Oxychloride 标题:Site Selectivity In The Reaction Of 3-Substituted Pyridine 1-Oxides With Phosphoryl Chloride 作者:Yamanaka,Hiroshi; Araki,Tomio; Sakamoto,Takao 参考文献:Chemical & Pharmaceutical Bulletin 日期:1988 卷标:36(6) 页码:2244-7
3-氰基-6-羟基吡啶置于n,N-二甲基甲酰胺 氯化亚砜体系中,用95%的收率获得产物6-氯-3-氰基吡啶 参考文献:Practical Synthesis Of (6-Chloro-3-Pyridyl)Methylamine By Highly Selective Hydrogenation Of 6-Chloro-3-Pyridinecarbonitrile With Improved Raney Nickel Catalyst 标题:Practical Synthesis Of (6-Chloro-3-Pyridyl)Methylamine By Highly Selective Hydrogenation Of 6-Chloro-3-Pyridinecarbonitrile With Improved Raney Nickel Catalyst 摘要:本文描述了一种实用合成(6-氯-3-吡啶基)甲胺(1)的方法,该化合物是新烟碱类杀虫剂的重要中间体,采用对6-氯-3-吡啶腈(4)进行高度选择性的加氢反应.使用改进的raney镍催化剂,该催化剂由低镍含量合金(镍38%,铝62%)制备,并在浸出铝后在水中进行热处理(98°C,2小时),对4的选择性加氢反应非常有效.使用该催化剂对4进行加氢反应是在乙醇-水 [6:1 (V/v)] 和氨气的条件下,于50oc和1.2-1.4 Kg Cm-2的氢气压力下进行的,最终得到1的产率为86%,并反应生成脱氯副产物3-吡啶基甲胺,产率为2%. DOI:10.1246/bcsj.73.1227
专利号:US-2016090360-A1 优先权日:2013-04-26 标题:Synthesis of bace inhibitors 发明人:FETTES ALEC; MARTY HANS-PETER; SCALONE MICHELANGELO 权利人:HOFFMANN LA ROCHE 摘要:The present invention provides a one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula (I), useful in processes to manufacture BACE inhibitors.
专利号:US-2024383853-A1 优先权日:2021-09-28 标题:Oximes and their use in treatment of gba-related diseases 发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH 权利人:ZEVRA DENMARK AS 摘要:The present invention relates to oximes, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.
专利号:US-2009170828-A1 优先权日:2006-06-12 标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
专利号:US-11279687-B2 优先权日:2010-09-03 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; YUEN PO-WAI 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
专利号:CA-2909136-A1 优先权日:2013-04-26 标题 :Synthesis of bace inhibitors
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.