CAS: 4023-02-3; 1H-Pyrazole-1-Carboximidamide Hydrochloride

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CAS号288-13-1 吡唑 | CAS号420-04-2 氰胺 | CAS号102-52-3 1,1,3,3-四甲氧基丙烷 | CAS号2582-30-1 氨基胍碳酸氢盐 | CAS号35877-22-6 1H-pyrazole,hyd... | CAS号1937-19-5 氨基胍盐酸盐 | CAS号14901-20-3 {[氨基(亚氨基)甲基]氨基}乙酸盐酸盐 | CAS号19196-09-9 diaminomethylid... | CAS号19097-97-3 decylguanidine ... | CAS号1866-59-7 2-hexylguanidine | CAS号19010-48-1 1,1'-(1,8-°Ctan... | CAS号19341-56-1 butylguanidine ... | CAS号2498-47-7 N-环己基胍盐酸盐 | CAS号289-95-2 嘧啶 | CAS号6659-35-4 6-胍基己酸 | CAS号330-69-8 1-benzyl-1-meth...

N-Boc-1H-吡唑-1-甲脒置于硫酸,Sodium Chloride体系中,用 Neat (No Solvent) 作为反应溶剂,化学反应 3.0H,以99%的收率获得产物1H-吡唑-1-甲脒盐酸盐
参考文献:通过异位反应生成氯化氢气体进行无溶剂 N-Boc 脱保护
标题:通过异位反应生成氯化氢气体进行无溶剂 N-Boc 脱保护
摘要:描述了一种有效,可扩展且可持续的方法,用于在无溶剂条件下使用低至接近化学计量的氯化氢气体对氨基甲酸叔丁酯 (N-Boc) 保护基团进行定量脱保护.我们展示了在两室反应器中从氯化钠和硫酸异位反应生成氯化氢气体,介绍了一种用于控制和化学计量释放 Hcl 气体的简单方法.无溶剂条件允许对多种n进行脱保护-Boc衍生物以定量产率获得盐酸盐.该程序消除了对任何后处理或纯化步骤的需要,为标准方法提供了一种简单的绿色替代方案.由于无溶剂,无水条件,该方法对酸敏感官能团具有高耐受性,并提供扩展的官能团正交性.
DOI:10.1039/d1Ob00728A

专利信息

专利号:US-2006264608-A1
优先权日:2001-08-03
标题 :Bi-directional synthesis of oligoguanidine transport agents
发明人：WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

专利号:US-7067698-B2
优先权日:2001-08-03
标 题 :Bi-directional synthesis of oligoguanidine transport agents
发明人：WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

专利号:US-2014073804-A1
优先权日:2011-02-24
标 题 :Process for the preparation of zanamivir
发明人：CHARAN GANPAT DAN SHIMBHU; TEHARE AJAY ONKARSINGH; SINGH KUMAR KEMLESH LAXMI
权利人:CHARAN GANPAT DAN SHIMBHU; TEHARE AJAY ONKARSINGH; SINGH KUMAR KEMLESH LAXMI
摘要:The present invention provides a process for preparing 5-(acetylamino)-4-[(aminoiminomethyl)amino]-2,6-anhydro-3,4,5-trideoxy-D-glycero-D-galacto-non-enonic acid Formula (I), which process comprises reducing compound of Formula (IV) by Lindlar catalyst in presence of hydrogen to obtain compound of Formula (V). reacting compound of Formula (V) with pyrazole-1H-carboxamidine or its suitable salt to obtain compound of Formula (VIII). hydrolyzing the compound of Formula (VIII) to give compound of Formula (I). The present invention also provides compounds of formula (VIII) which may be used in the synthesis of zanamivir. The present invention also provides process for preparing compound of formula (VIII) and process involving the use of Formula (VIII), including in the synthesis of zanamivir.

专利号:US-7834174-B2
优先权日:2004-09-10
标 题 :Per-6-guanidino-, alkylamino-cyclodextrins, methods of their synthesis and their use for the compaction of DNA and intercellular delivery
发明人：MAVRIDIS IRENE M; YANNAKOPOULOU KONSTANTINA; ELIADOU KYRIAKI; MOURTZIS NIKOLAOS; AGGELIDOU CHRYSI
权利人:MAVRIDIS IRENE M; YANNAKOPOULOU KONSTANTINA; ELIADOU KYRIAKI; MOURTZIS NIKOLAOS; AGGELIDOU CHRYSI
摘要:The invention relates to new compounds of type hexakis(6-deoxy-6-NH(CH 2 ) n —R 1 )α-cyclodextrin and heptakis(6-deoxy-6-NH(CH 2 ) n —R 1 )-(β-cyclodextrin, and octakis(6-deoxy-6-NH(CH 2 ) n —R 1 )-γ-cyclodextrin, where n=2-6 when R 1 =NH 2 and n=0 when R 1 =C(â•?NH)NH 2 and n=2-6 when R 1 =NH—C(â•?NH)NH 2 and their use in the compaction of DNA and in cell permeation. The invention also relates to methods of synthesis of the above compounds.

专利号:US-8178672-B2
优先权日:2004-10-19
标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
发明人：ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC
权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC
摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.

专利号:US-8653282-B2
优先权日:2007-10-18
标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein
发明人：FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G
权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT
摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.