Processes for preparation of organic compounds
    3.
    发明授权
    Processes for preparation of organic compounds 失效
    有机化合物的制备方法

    公开(公告)号:US07358356B2

    公开(公告)日:2008-04-15

    申请号:US10529392

    申请日:2003-10-02

    IPC分类号: C07D499/18

    CPC分类号: C07D499/893 C07D499/88

    摘要: The present invention provides a method for preparing an organic compound, which comprises a dehydration step of distilling off water from a polar organic solvent solution containing the organic compound and water to bring the concentration of water below a given level, wherein the dehydration step comprises distilling off water together with the polar organic solvent while adding a polar organic solvent to the solution, or comprises repeating several cycles of adding a polar organic solvent to the solution and then distilling off water together with the polar organic solvent. The present invention further provides the preparation of an organic compound, which enables efficient isolation of the target product in high isolated yield from a polar organic solvent solution containing the organic compound, water and, if necessary, a compound which produces, upon coming into contact with water or the like, a substance accelerating the decomposition of the organic compound.

    摘要翻译: 本发明提供了一种制备有机化合物的方法,该方法包括从含有有机化合物和水的极性有机溶剂溶液中蒸馏出水以使水的浓度低于给定水平的脱水步骤,其中脱水步骤包括蒸馏 将极性有机溶剂与极性有机溶剂一起加入到溶液中,或者包括重复多次向溶液中加入极性有机溶剂,然后与极性有机溶剂一起蒸馏出水。 本发明还提供有机化合物的制备,其能够以高分离产率从含有有机化合物的极性有机溶剂溶液,水和必要时的化合物在接触时产生高分离产物。 用水等加速有机化合物分解的物质。

    Antibacterial penem esters derivatives
    5.
    发明授权
    Antibacterial penem esters derivatives 失效
    抗菌青蒿酯衍生物

    公开(公告)号:US5885981A

    公开(公告)日:1999-03-23

    申请号:US470944

    申请日:1995-06-06

    CPC分类号: C07D499/88

    摘要: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a hydrogen atom or linear or branched C.sub.1 --C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.

    摘要翻译: 抗生素penem化合物由下式表示:其中R表示下列通式的基团:其中R 1为氢原子或直链或支链C 1 -C 6烷基,R 2为特定的取代或未取代的 烷基,芳基或芳烷基,n为1-6的整数,Y为其环中具有1或2个氧原子的5或6元杂环脂族基团,Z为特定的5-取代的2-氧代 -1,3-二氧杂环戊烯-4-基。 还描述了用于口服给药的抗生素组合物。

    Azetidinone compounds useful in the preparation of carbapenem
antibiotics and process for preparing carbapenem and penem compounds
    7.
    发明授权
    Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds 失效
    可用于制备碳青霉烯类抗生素的氮杂环丁酮化合物及其制备碳青霉烯和青霉烯化合物的方法

    公开(公告)号:US5541317A

    公开(公告)日:1996-07-30

    申请号:US289133

    申请日:1994-08-11

    摘要: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; is R.sup.4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds. Penem and carbapenem compounds having a group of formula --SA' are prepared from a corresponding compound having a substituted thio, sulfinyl or sulfonyl group at this position by reaction with a compound A'SH (where A' is an organic group) in the presence of a salt of a metal of Group II or III of the Periodic Table.

    摘要翻译: 式(I)的化合物:其中:R1是氢或羟基保护基; R 2是烷基,烷氧基,卤素,任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基,任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基,其中Y是氧或硫,R 5和R 6各自是烷基,芳基或芳烷基,或者R 5和R 6以及它们 一起形成杂环基; 是R 4氢或氨基保护基; Z为硫或氧; 是制备碳青霉烯化合物的有价值的中间体,并且在转化成这种碳青霉烯化合物期间保留期望的构型。 在具有取代的硫代,亚磺酰基或磺酰基的相应化合物的化合物A'SH(其中A'为有机基团)的存在下,通过与化合物A'SH(其中A'为有机基团)反应,由具有取代的硫代,亚磺酰基或磺酰基的相应化合物制备具有式-SA'基团的Penem和carbapenem化合物 的元素周期表II或III族金属的盐。