Alpha,beta-substituted acroleins and their preparation
    4.
    发明授权
    Alpha,beta-substituted acroleins and their preparation 失效
    α,β-取代的丙烯醛及其制备方法

    公开(公告)号:US4723042A

    公开(公告)日:1988-02-02

    申请号:US005691

    申请日:1987-01-22

    摘要: Alpha,beta-substituted acroleins of the general formula I ##STR1## where A and B are identical or different and are each C.sub.1 -C.sub.4 -alkyl, naphthyl, biphenyl or phenyl which may be monosubstituted or polysubstituted by halogen, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, phenoxy or phenylsulfonyl, are prepared by a process in which a compound of the general formula III ##STR2## where A has the above meanings and R.sup.1 and R.sup.2 are identical or different and are each C.sub.1 -C.sub.4 -alkyl or together possess the carbon atoms required to complete a ring, is reacted with a phosphorus compound of the general formula IV or V ##STR3## where B the meanings stated above, R.sup.1 and R.sup.2 are as defined above and X.sup..crclbar. is a halide ion, in the presence of a base. The alpha,beta-substituted acroleins can be further processed to give hydroxymethyloxiranes.

    摘要翻译: α,β取代的通式I(I)的丙烯醛,其中A和B是相同或不同的并且各自是可被卤素,硝基, C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4卤代烷基,苯氧基或苯基磺酰基,其中A为具有上述含义的通式III(III)的化合物和R 1 和R 2相同或不同,并且各自为C 1 -C 4 - 烷基或一起具有完成环所需的碳原子,与通式IV或V所示的磷化合物反应,其中B为上述含义,R 1 和R 2如上所定义,并且X( - )是卤素离子,在碱的存在下。 α,β-取代的丙烯醛可以进一步加工得到羟基甲基环氧乙烷。

    Alpha, beta-substituted acroleins
    5.
    发明授权
    Alpha, beta-substituted acroleins 失效
    α,β-取代的丙烯醛

    公开(公告)号:US4804785A

    公开(公告)日:1989-02-14

    申请号:US97113

    申请日:1987-09-16

    摘要: Alpha,beta-substituted acroleins of the general formula I ##STR1## where A and B are identical or different and are each C.sub.1 -C.sub.4 -alkyl, naphthyl, biphenyl or phenyl which may be monosubstituted or polysubstituted by halogen, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, phenoxy or phenylsulfonyl, are prepared by a process in which a compound of the general formula III ##STR2## where A has the above meanings and R.sup.1 and R.sup.2 are identical or different and are each C.sub.1 -C.sub.4 -alkyl or together possess the carbon atoms required to complete a ring, is reacted with a phosphorus compound of the general formula IV or V ##STR3## where B the meanings stated above, R.sup.1 and R.sup.2 are as defined above and X.sup..crclbar. is a halide ion, in the presence of a base. The alpha,beta-substituted acroleins can be further processed to give hydroxymethyloxiranes.

    摘要翻译: α,β取代的通式I(I)的丙烯醛,其中A和B是相同或不同的并且各自是可被卤素,硝基, C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4卤代烷基,苯氧基或苯基磺酰基,其中A为具有上述含义的通式III(III)的化合物和R 1 和R 2相同或不同,并且各自为C 1 -C 4烷基或一起具有完成环所需的碳原子,与通式IV或V的磷化合物反应(V) )其中B为上述含义,R1和R2如上所定义,X( - )为卤素离子,在碱的存在下。 α,β-取代的丙烯醛可以进一步加工得到羟基甲基环氧乙烷。

    Preparation of alkyl O,O-dialkyl-.gamma.-phosphonotiglates
    6.
    发明授权
    Preparation of alkyl O,O-dialkyl-.gamma.-phosphonotiglates 失效
    烷基O,O-二烷基-γ-膦酸吡啶的制备

    公开(公告)号:US4937308A

    公开(公告)日:1990-06-26

    申请号:US205283

    申请日:1988-06-10

    IPC分类号: C07F9/40

    CPC分类号: C07F9/4015

    摘要: Alkyl .gamma.-halotiglates of the general formula I ##STR1## where X is Cl or Br and R.sup.2 is alkyl of 1 to 3 carbon atoms, having a high E isomer content, are prepared by a process in which(a) the corresponding 2-methyl-but-3-enoate of the general formula II ##STR2## is reacted with chlorine or bromine in the absence of a solvent and (b) the resulting 2-methyl-3,4-dihalobutyrate of the general formula III ##STR3## is dehydrohalogenated by reaction with a solution of an alkali metal hydroxide in an alcohol R.sup.2 OH, where R.sup.2 has the stated meaning, or in a mixture of water and an alcohol R.sup.2 OH, and the products are further processed to give O,O-dialkyl-.gamma.-phosphonotiglates of the general formula IV ##STR4## where R.sup.1 is alkyl of 1 to 4 carbon atoms and R.sup.2 is alkyl of 1 to 3 carbon atoms, preferably ethyl, by reaction with a trialkyl phosphite and thermal isomerization. The process gives C.sub.5 building blocks which are extremely interesting for polyene chemistry, the said building blocks being obtained in good yields and essentially in the form of the required E isomers.

    摘要翻译: 通过以下方法制备通式I的烷基γ-卤代吡咯烷酮,其中X是Cl或Br,R2是具有高E异构体含量的1至3个碳原子的烷基,其中(a) 在不存在溶剂的情况下,使通式II(II)的相应的2-甲基 - 丁-3-烯酸酯与氯或溴反应,和(b)所得的2-甲基-3,4-二卤代丁酸酯 通过与碱金属氢氧化物在醇R2OH中的溶液(其中R2具有所述含义)或在水和醇R2OH的混合物中进行反应脱卤化氢,并将产物进一步加工 得到通式IV(IV)的O,O-二烷基-γ-膦腈吡咯烷酮,其中R 1为1至4个碳原子的烷基,R 2为1至3个碳原子的烷基,优选为乙基,通过与 亚磷酸三烷基酯和热异构化。 该方法提供了对多烯化学非常有趣的C5构建块,所述构建块以良好的产率获得并且基本上以所需的E异构体的形式获得。

    Method for the production of biperidin
    8.
    发明授权
    Method for the production of biperidin 失效
    生产丁吡啶的方法

    公开(公告)号:US07030247B2

    公开(公告)日:2006-04-18

    申请号:US10477761

    申请日:2002-05-17

    IPC分类号: C07D211/06

    CPC分类号: C07D295/088 C07D295/108

    摘要: The invention relates to a method for the production of biperiden by reacting an exo/endo mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone with a phenyl magnesium compound to form an isomer mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-piperidino-1-propanol, whereby biperiden is obtained therefrom by conversion of said mixture into corresponding hydrochloride, isolation of said hydrochloride, reconversion to the free base and crystallization of said biperiden.

    摘要翻译: 本发明涉及一种通过使1-(双环[2.2.1]庚-5-烯-2-基)-3-哌啶子基-1-丙酮的外部/内部混合物与 苯基镁化合物形成1-(双环[2.2.1]庚-5-烯-2-基)-1-苯基-3-哌啶-1-基-1-异丙醇的异构体混合物,由此通过转化得到二哌啶 的所述混合物转化成相应的盐酸盐,分离所述盐酸盐,重新转化为游离碱并结晶所述双倍哌啶。

    Method for producing atropic acid ethyl ester
    9.
    发明授权
    Method for producing atropic acid ethyl ester 有权
    生产阿托酸乙酯的方法

    公开(公告)号:US06509493B1

    公开(公告)日:2003-01-21

    申请号:US09743894

    申请日:2001-01-17

    IPC分类号: C07C6976

    CPC分类号: C07C67/343 C07C69/618

    摘要: A process for preparing ethyl atropate by reacting ethyl phenylacetate with paraformaldehyde in the presence of a base is described and entails employing as ethyl phenylacetate a product which contains not more than 0.03% of the corresponding methyl phenylacetate, and carrying out the reaction in N-methyl-pyrrolidone or N,N-dimethylformamide.

    摘要翻译: 描述了通过在碱存在下使苯乙酸乙酯与多聚甲醛反应来制备乙酸乙酯的方法,并且需要使用苯乙酸乙酯作为相应的苯基乙酸苯酯不超过0.03%的产物,并在N-甲基 - 吡咯烷酮或N,N-二甲基甲酰胺。