CAS: 51322-75-9; 5-Chloro-N-(4,5-Dihydro-1H-Imidazol-2-yl)Benzo[c][1,2,5]Thiadiazol-4-Amine

该化合物是一种肌肉放松剂,主要用于管理与多发性硬化和脊髓损伤等条件有关的聚变,它作为阿尔法-2抗性激素活性剂发挥作用,这意味着抑制释放刺激性...

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上下游产品

1-acetylimidazolidin-2-one 4-amino-5-chloro-2,1,3-benzothiadiazole 4,5-dihydro-1H-imidazole-2-sulfonic acid 2-chloro-2-imidazoline hydr°Chloridetizanidine hydr°Chloride

合成工艺路线路线简述

  • 合成目标产物 Tizanidine 主要起始原料 4-Amino-5-Chloro-2,1,3-Benzothiadiazole And 1H-Imidazole, 2-Chloro-4,5-Dihydro-, Hydrochloride (1:1)
  • (文献来源)合成步骤主要原料 4-Amino-5-Chloro-2,1,3-Benzothiadiazole 和 1H-Imidazole, 2-Chloro-4,5-Dihydro-, Hydrochloride (1:1)
4-氨基-5-氯-2,1,3-苯并噻二唑置于水,Sodium Hydroxide,三氯氧磷体系中,用 甲醇,丙酮 作为反应溶剂,化学反应 22.0H,反应生成 替扎尼定
参考文献:咪唑啉间二氮杂环戊烯衍生物的制备方法
标题:咪唑啉间二氮杂环戊烯衍生物的制备方法
摘要:本发明公开了一种咪唑啉间二氮杂环戊烯衍生物的制备方法,具体涉及盐酸替扎尼定的制备方法,包括以下步骤:A,取化合物ii和化合物iii,在有机溶剂中,脱水剂存在下反应,然后经碱化,过滤,即得化合物iv;b,以步骤a所得化合物iv为原料,经水解,制备得到式v所示替扎尼定;c,以步骤b所得替扎尼定为原料制备得到式i所示盐酸替扎尼定.本发明方法同时具有较高的产率和纯度,并且操作简便,生产效率高,环保,安全,适用于工业化大生产,具有广阔的市场应用前景.

海关参考信息

专利信息


专利号:US-2011028688-A1
优先权日:2006-06-21
标 题 :Crystal structure of ox40l and ox40l complexed with ox40 receptor
发明人:HYMOWITZ SARAH; COMPAAN MCGUINN DEANNE
权利人:GENENTECH INC
摘要:The present disclosure provides crystals of and structural coordinates of mOX40L, hOX40L, hOX40 receptor and complexes thereof. The crystals and crystal structures are useful, for example, in the design and synthesis of modulators of mOX40L, hOX40L, and/or hOX40 receptor.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

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; KLÜNDER 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; KLÜNDER 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; KLÜNDER 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).

专利号:US-7799829-B2
优先权日:2006-07-28
标 题 :Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
发明人:DAI XUEDONG; GANGAKHEDKAR ARCHANA; XIANG JIA-NING; GALLOP MARK A
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.
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合成参考文献


参考文献:10.1007/s00484-009-0300-x
摘要:Matsumoto S, Shimodozono M, Etoh S, Shimozono Y, Tanaka N, Kawahira K. Beneficial effects of footbaths in controlling spasticity after stroke. International Journal of Biometeorology. 2010 Feb 17;54(4):465–73. doi: 10.1007/s00484-009-0300-x.
参考文献:10.1007/s00228-005-0028-4
摘要:Zesiewicz TA, Pathak A, Sullivan KL, Shamayev M, Hauser RA. Treatment of chorea with levetiracetam. European Journal of Clinical Pharmacology. 2005 Dec 01;62(1):87. doi: 10.1007/s00228-005-0028-4.
参考文献:10.1107/s1600536811008348
摘要:John P, Khan IU, Akkurt M, Ramzan MS, Sharif S. 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine (tizanidine). Acta Crystallogr E Struct Rep Online. 2011 Mar 12;67(4):o838–9. doi: 10.1107/s1600536811008348.
参考文献:10.1155/2011/403808
摘要:Handy CR, Krudy C, Boulis N, Federici T. Pain in Amyotrophic Lateral Sclerosis: A Neglected Aspect of Disease. Neurology Research International. 2011;2011():1–8. doi: 10.1155/2011/403808.
参考文献:10.1111/j.1526-4610.2011.01956.x
摘要:Aurora SK. Implications of current clinical trials focused on medication overuse and therapeutic prophylaxis. Headache. 2011 Jul;51 Suppl 2():93–100. doi: 10.1111/j.1526-4610.2011.01956.x.
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