CAS: 747-36-4; 2-((4-((7-Chloroquinolin-4-yl)Amino)Pentyl)(Ethyl)Amino)Ethanol Sulfate

上下游产品

hydroxychloroquine 4,7-dichloroquinoline -2-pentanaminerac-5--2-pentanamine (S)-Hydroxychloroquine

硫酸羟氯喹置于硫酸体系中,用 乙醇 作为反应溶剂,以93 %的收率获得产物硫酸羟基氯喹
参考文献:浓条件下高产合成羟氯喹的工艺:二甲亚砜促进或3,5-双(三氟甲基)苯酚催化氯吡啶的亲核胺化
标题:浓条件下高产合成羟氯喹的工艺:二甲亚砜促进或3,5-双(三氟甲基)苯酚催化氯吡啶的亲核胺化
摘要:我们的目标是开发合成抗疟药物羟氯喹的替代途径,我们的努力导致开发了氯吡啶与胺(即苯胺,哌啶,环己胺和炔丙胺)的亲核芳香取代(sn Ar)反应的两种互补方法.其中一种被认为是通过溶剂效应促进dmso,而另一种方法采用3,5-双(三氟甲基)苯酚作为催化剂.在前一种情况下,我们发现 Dmso 的用量对于获得高产率至关重要.1.00 当量的 Dmso 被确定为实现最高产率的最佳量.然而,在后一种情况下,发现催化量的 3,5-双(三氟甲基)苯酚(50-40 Mol%)对 S N Ar具有高活性,从而以高产率提供相应的氨基吡啶高达98%.实验结果和x射线晶体学表明后者发生了加成-消除机制.
DOI:10.1021/acs.Oprd.3C00220

专利信息

专利号:WO-2012149093-A1
优先权日:2011-04-26
标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof
发明人：LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.

专利号:WO-2021068203-A1
优先权日:2019-10-11
标 题 :Use of chloroquine or derivative hydroxychloroquine
发明人：LI YANBING; GUO YAN; LI HAI; CHEN XUEYING; CHEN YUXIN; GUAN HONGYU; LIU LIEHUA; XIAO HAIPENG
权利人:1ST AFFILIATED HOSPITAL SUN YAT SEN UNIV
摘要:Use of chloroquine or a derivative thereof hydroxychloroquine in the preparation of a medicament for the treatment of Graves' oculopathy. Chloroquine or the derivative thereof hydroxychloroquine has a significant inhibitory effect on the overproliferation, adipogenic differentiation and hyaluronic acid synthesis of fibroblasts.

专利号:US-2006287257-A1
优先权日:2005-06-20
标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium
发明人：STOCKEL RICHARD F
权利人:STOCKEL RICHARD F
摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.

专利号:US-11993606-B2
优先权日:2015-10-16
标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÃœNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

专利号:US-11976077-B2
优先权日:2015-10-16
标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof
发明人：PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÃœNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.

专利号:US-11512092-B2
优先权日:2015-10-16
标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÃœNDER BEN
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).