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    Copper catalyzed process for producing 4-substituted azetidinone derivatives
    2.
    发明授权
    Copper catalyzed process for producing 4-substituted azetidinone derivatives 失效
    用于生产4-取代的氮杂环丁酮衍生物的铜催化方法

    公开(公告)号：US5808055A

    公开(公告)日：1998-09-15

    申请号：US498499

    申请日：1995-07-05

    Applicant: Masashi Nakajima, deceased ,  Yasuharu Kimura ,  Kiyohito Imai

    Inventor： Masashi Nakajima, deceased ,  Yasuharu Kimura ,  Kiyohito Imai

    IPC: C07D201/02 ,  C07D205/09 ,  C07D403/12 ,  C07D405/12 ,  C07F7/18

    CPC classification number: C07D403/12 ,  C07D201/02 ,  C07D205/09 ,  C07D405/12

    Abstract: A process for producing a 4-substituted azetidinone derivative represented by the following general formula �III!: ##STR1## (wherein OR is a protected hydroxy group, Y is an alkyl group, an alkoxy group, a silyloxy group, a carbamoyloxy group, an amino group, a substituted or unsubstituted aromatic group or a substituted or unsubstituted heterocyclic group, and n is an integer of 0 or 1, provided that n does not represent 0 when Y is an alkoxy group, silyloxy group, carbamoyloxy group or amino group), characterized in that a 2-azetidinone derivative represented by the following general formula �I!: ##STR2## (wherein OR is as defined above, and X is an alkyl group or a substituted or unsubstituted aromatic group) is reacted with thiocarboxylic acid represented by the following general formula �II!: HSCO--(CH.sub.2).sub.n --Y �II! (wherein Y and n are respectively as defined above) in an organic solvent in the presence of copper compounds.

    Abstract translation: 用于制备由以下通式[III]表示的4-取代的氮杂环丁酮衍生物的方法：其中OR为被保护的羟基，Y为烷基，烷氧基，甲硅烷氧基， 氨基甲酰氧基，氨基，取代或未取代的芳基或取代或未取代的杂环基，并且n为0或1的整数，条件是当Y为烷氧基时，n不为0，甲硅烷氧基，氨基甲酰氧基 或氨基），其特征在于由以下通式[I]表示的2-氮杂环丁酮衍生物：其中OR如上所定义，X为烷基或取代或未取代的芳族基团 ）与铜化合物存在下的有机溶剂中由以下通式[II]表示的硫代羧酸反应：HSCO-（CH 2）n Y [II]（其中Y和n分别如上定义）。

    Process of synthesizing N-acyl auxiliaries
    3.
    发明授权
    Process of synthesizing N-acyl auxiliaries 失效
    合成N-酰基助剂的方法

    公开(公告)号：US5594134A

    公开(公告)日：1997-01-14

    申请号：US414541

    申请日：1995-03-31

    Applicant: Guo-Jie Ho ,  David J. Mathre

    Inventor： Guo-Jie Ho ,  David J. Mathre

    IPC: C07D201/02 ,  C07D205/04 ,  C07D207/12

    CPC classification number: C07D201/02

    Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.

    Abstract translation: 公开了合成N-酰基辅助化合物的方法。 在锂盐和胺碱的存在下，使下式的化合物与一种酸酐反应得到N-酰化的辅助物。

    Preparation of 5-membered ring heterocycles
    4.
    发明授权
    Preparation of 5-membered ring heterocycles 失效
    五元环杂环的制备

    公开(公告)号：US5453516A

    公开(公告)日：1995-09-26

    申请号：US165463

    申请日：1993-12-13

    Applicant: Rolf Fischer ,  Rolf Pinkos

    Inventor： Rolf Fischer ,  Rolf Pinkos

    IPC: C07D201/02 ,  C07D207/26 ,  C07D207/267 ,  C07D307/33 ,  C07D315/00 ,  C07D207/27 ,  C07D307/28

    CPC classification number: C07D201/02 ,  C07D207/267 ,  C07D307/33 ,  C07D315/00

    Abstract: A process for preparing 5-membered ring heterocycles of the general formula I ##STR1## where R.sup.1 is methyl or hydroxyethyl,R.sup.2,R.sup.3,R.sup.4,R.sup.5 and R.sup.6 are hydrogen, C.sub.1 - to C.sub.12 -alkyl, C.sub.2 - to C.sub.12 -alkenyl, aryl, C.sub.3 - to C.sub.8 -cycloalkyl, C.sub.1 - to C.sub.12 -alkoxy, halogen, C.sub.2 - to C.sub.20 -alkoxycarbonylalkyl, C.sub.2 - to C.sub.20 -alkylcarbonyloxy, formyl, C.sub.2 - to C.sub.20 -formylalkyl, benzoyl or --CH(OR.sup.3)(OR.sup.5), or R.sup.3 and R.sup.5 together are a C.sub.2 - to C.sub.7 -alkylene chain which is unsubstituted or monosubstituted to pentasubstituted by R.sup.4 or a .dbd.CH--CH.dbd.CH--CH.dbd. unit which is unsubstituted or monosubstituted to tetrasubstituted by R.sup.4,X is oxygen or N--R.sup.4by reacting 5-membered ring heterocycles of the general formula II ##STR2## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the abovementioned meanings and Y is hydrogen, acetyl or C.sub.2 - to C.sub.20 -alkoxycarbonyl, with dimethyl or ethylene carbonate in the presence of a nitrogen-containing base at from 50.degree. to 300.degree. C. and from 0.01 to 50 bar is described.

    Abstract translation: 其中R 1是甲基或羟乙基，R 2，R 3，R 4，R 5和R 6是氢，C 1 -C 12 - 烷基，C 2 -C 12的通式I（I）的五元环杂环的制备方法 - 烯基，芳基，C 3 -C 8 - 环烷基，C 1 -C 12 - 烷氧基，卤素，C 2 -C 20 - 烷氧基羰基烷基，C 2 -C 20 - 烷基羰氧基，甲酰基，C 2 -C 20甲酰烷基，苯甲酰基或-CH ）（OR 5）或R 3和R 5一起是未被取代或单取代以被R4或a = CH-CH = CH-CH =未被R4单取代或单取代的单元的C2至C7-亚烷基链， X是通过使通式II的5-元环杂环（II）其中R 2，R 3，R 4，R 5，R 6和X具有上述含义并且Y是氢，乙酰基或C 2 - 在含有50〜300℃的含氮碱和0.01〜50巴的存在下，与二甲基或碳酸亚乙酯进行反应。

    Process for preparing lower lactams from allylic amine substrates
    6.
    发明授权
    Process for preparing lower lactams from allylic amine substrates 失效
    从烯丙基胺底物制备低级内酰胺的方法

    公开(公告)号：US4111952A

    公开(公告)日：1978-09-05

    申请号：US745018

    申请日：1976-11-26

    Applicant: John F. Knifton

    Inventor： John F. Knifton

    IPC: C07D201/02 ,  C07D207/26

    CPC classification number: C07D201/02

    Abstract: This invention concerns processes for preparing cyclic, 5-membered ring, lactams through the carbonylation of allylic substrates in the presence of rhodium catalysts.

    Abstract translation: 本发明涉及在铑催化剂存在下通过烯丙基底物的羰基化制备环状5元环，内酰胺的方法。

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