CAS: 5575-21-3; (6R,7R)-3-[(4-Carbamoylpyridin-1-Ium-1-yl)Methyl]-8-Oxo-7-[(2-Thiophen-2-Ylacetyl)Amino]-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylate

上下游产品

2-thienylacetic acid chloride isonicotinamide 7-Amin°Cephalosporanic acid cephalothin

头孢噻吩置于盐酸,双氧水,六甲基二硅氮烷,N,N-二乙基苯胺体系中,用 甲醇,二氯甲烷,水 作为反应溶剂,化学反应 16.5H,反应生成 头孢洛宁
参考文献:一种头孢洛宁的制备方法
标题:一种头孢洛宁的制备方法
摘要:本发明涉及一种头孢洛宁的制备方法,该方法是以头孢噻吩酸和异烟酰胺为原料,在低温下反应得到产品.头孢噻吩酸溶解在有机溶剂中,利用硅烷化保护试剂进行羧基保护,继而与三甲基碘硅烷发生碘代反应;然后与异烟酰胺进行胺化反应,最后经醇解脱保护,低温下调节ph析晶得到头孢洛宁.本发明在有机溶剂中选择硅烷化试剂保护头孢噻吩酸,继而与三甲基碘硅烷反应,反应时间短,条件温和,反应完全,几乎无副反应发生;采用混合溶剂结晶方法,可以达到干燥快,颜色浅,收率高的特点,另外溶剂可以回收,减少污水的量,具有明显的经济效益和环境效益,有利于实现工业化生产.

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: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-9066864-B2
优先权日:2011-01-12
标 题:Use of liquid medium exchange by cross flow filtration in the preparation of drug suspensions
发明人：NIEDERMANN HANS PETER; BOTHE HEIKO
权利人:NIEDERMANN HANS PETER; BOTHE HEIKO; INTERVET INC
摘要:Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.

专利号:US-2025002508-A1
优先权日:2020-05-05
标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
发明人：HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
权利人:QPEX BIOPHARMA INC
摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

专利号:WO-9740034-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:JP-2000508664-A
优先权日:1996-04-22
标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes