CAS: 140-28-3; N1,N2-Dibenzylethane-1,2-Diamine

该化合物是属于苯基酯类的化学化合物,主要被确认为一种长效的青霉素,特别是用于治疗各种细菌感染,包括风湿热和梅毒的青霉素-青霉素-G.本扎提因的特征是白色到非白色的晶状粉,在水中溶解,但在有机溶剂中溶解.该化合物表现出相对较低的毒性特征,适合治疗用途.其药用动力特性允许长期释放和持续治疗效果,在临床环境中是有利的.此外,对苯并丁进行的其他领域的潜在应用,包括作为药物配方的防腐剂.

结构式图片

相似化合物

122-75-8 110-70-3 110-72-5

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

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合成工艺路线路线简述

  • 4556-23-4 + 26973-80-8 + 39556-13-3 = 140-28-3 + 21593-23-7
    反应条件:1.1 Reagents: Triethylamine Solvents: Methanol,Acetone,Water; 2 - 5 °C1.2 5 H,5 - 10 °C1.3 Reagents: Sodium Bicarbonate,Sodium Thiosulfate Solvents: Water1.4 6 H,37 - 40 °C
    标题:Method For Preparing Cephapirin Benzathine From Bromoacetyl 7-Amino Cephalosporanic Acid
    参考文献:China]

    27230-51-9 + 140-28-3 + 957-68-6 = 140-28-3 + 21593-23-7
    反应条件:1.1 Reagents: Triethylamine Solvents: Acetone,Water; 3 H,Ph 8 - 9,10 °C1.2 Solvents: Water; 6 H,37 - 40 °C
    标题:Improved Method For Synthesis Of Cephapirin Benzathine
    参考文献:China]

    4556-23-4 + 26973-80-8 + 140-28-3 = 140-28-3 + 21593-23-7
    反应条件:1.1 Reagents: Triethylamine Solvents: Methanol,Acetone,Water; 2 - 5 °C; 5 H,0 - 5 °C1.2 Reagents: Sodium Bicarbonate,Sodium Thiosulfate Solvents: Water; 30 Min,0 - 5 °C1.3 6 H,37 - 40 °C
    标题:Synthesis Of Cephapirin Benzathine
    作者:Fu,Haiyan; Tian,Meiru
    参考文献:Zhongguo Yiyao Gongye Zazhi 日期:2009 卷标:40(10)
1,2-Dibenzyl-1,2-Diazetin-3-One置于b2H6-Thf体系中,化学反应 2.0H,以85%的收率获得n,N'-二苄基乙二胺
参考文献:光化学环收缩法合成1,2-二氮杂环丁酮(氮杂-β-内酰胺)
标题:光化学环收缩法合成1,2-二氮杂环丁酮(氮杂-β-内酰胺)
摘要:在醇,二乙胺或水的存在下辐照4-重氮吡唑烷-3,5-二酮(11)产生1,2-二氮杂二酮(12),其通过光化学wolff重排与环收缩形成,然后使所得的烯酮与亲核试剂.在双环重氮化合物(11D)的情况下,断裂反应与环收缩竞争.氮杂-β-内酰胺(12)在其红外光谱中显示出预期的高频羰基拉伸.酸(12E)易于脱羧得到4-未取代的1,2-二苄基二氮杂二酮(28),其四元环通过碱水解,氢化铝锂或乙硼烷裂解得到(29),(30)和(31)(方案9).将(12E)的羧基取代基修饰成酰氨基的尝试是失败的.
Doi:10.1039/p19870000877

海关参考信息

专利信息


专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-2016031800-A1
优先权日:2013-03-14
标 题:Synthesis of chiral kynurenine compounds and intermediates
发明人:TRETYAKOV ALEXANDER; DROUET KEITH E; SANDERS WILLIAM
权利人:VISTAGEN THERAPEUTICS INC
摘要:Provided are methods for the synthesis of compounds including chiral kynurenine compounds, intermediates useful for the synthesis thereof, and related compounds. For example, methods are provided for the synthesis of L-4-chlorokynurenine.

专利号:US-2012165520-A1
优先权日:2010-12-23
标题:Process for the synthesis of prodrugs of opioids
发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人:DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人:DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
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