Method for the production of ceftobiprole medocaril
    2.
    发明授权
    Method for the production of ceftobiprole medocaril 有权
    生产头孢匹隆中间体的方法

    公开(公告)号:US09139597B2

    公开(公告)日:2015-09-22

    申请号:US13320430

    申请日:2010-05-25

    摘要: The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.

    摘要翻译: 本发明涉及一种生产有机化合物的方法,特别是(6R,7R)-7 - [(Z)-2-(5-氨基 - [1,2,4]噻二唑-3-基) -2-羟基亚氨基 - 乙酰氨基] -8-氧代-3 - [(E) - (R)-1' - (5-甲基-2-氧代 - [1,3] - 二氧杂环戊烯-4-基甲氧基羰基)-2- 氧基 - [1,3']联吡咯烷基-3-亚基甲基] -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸酯(头孢噻肟中间体)和通式( 1)和通式(2),本发明的生产中的化合物本身和中间体。

    Carbonyl Asymmetric Alkylation
    5.
    发明申请
    Carbonyl Asymmetric Alkylation 有权
    羰基不对称烷基化

    公开(公告)号:US20110009648A1

    公开(公告)日:2011-01-13

    申请号:US12223096

    申请日:2007-01-22

    摘要: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

    摘要翻译: 本发明涉及羰基的立体选择性烷基化方法和中间体。 本发明特别允许立体选择性制备抗抑郁药物依他普仑。 已经发现硼酸或硼酸衍生物是用于将手性基团连接到含有待烷基化羰基的化合物的有用的桥连元件。 因此,所述硼酸盐和硼酸盐可用于在含有羰基和能够与硼酸或硼酸衍生物反应的锚定基团的化合物中羰基的不对称烷基化方法。 不对称烷基化可以通过将待烷基化的羰基和能够与硼酸或硼酸衍生物反应的锚定基团与硼酸或硼酸衍生物反应,加入手性醇,并加入有机金属化合物 。 在烷基化反应之后,可以通过水解容易地除去硼酸盐和硼酸盐。

    Purification process
    8.
    发明授权
    Purification process 失效
    净化过程

    公开(公告)号:US06313289B1

    公开(公告)日:2001-11-06

    申请号:US09341542

    申请日:1999-08-04

    IPC分类号: C07D50104

    CPC分类号: C07D501/00

    摘要: Crystalline 2-(amninothiazol-4-yl)-2-(tert.butoxycarbonylmethoxyimino)acetic acid-S-mercapto-benzo-thiazolylester in form of an N,N-dimethylacetamide solvate; a crystalline salt of a 7-[2-(aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid with an amine of formula N(R1)(R2)(R3), wherein R1, R2, and R3 have various meanings, a crystalline sulphuric acid addition salt of a 7-[2-(2-aminothiazol-4-yl)-2-carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid; and the use of these salts in the production of cefixime, e.g. in form of a trihydrate.

    摘要翻译: N,N-二甲基乙酰胺溶剂化物形式的2-(氨基噻唑-4-基)-2-(叔丁氧基羰基甲氧基亚氨基)乙酸S-巯基 - 苯并噻唑酯的结晶; 7- [2-(氨基噻唑-4-基)-2-(羧基甲氧基亚氨基)乙酰氨基] -3-乙烯基-3-头孢烯-4-羧酸与式N(R1)(R2)的胺的结晶盐, (R3),其中R1,R2和R3具有各种含义,7- [2-(2-氨基噻唑-4-基)-2-羧甲氧基亚氨基)乙酰氨基] -3-乙烯基-3 - 头孢-4-羧酸; 以及这些盐在头孢克肟的生产中的用途。 呈三水合物的形式。