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    • 5. 发明申请
    • METHOD FOR THE ENANTIOMER SEPARATION OF CIS-8-BENZYL-7,9-DIOXO-2,8-DIAZABICYCLO[4.3.0]NONANE
    • 方法光学CIS-8-苄基-7,9-二氧代-2,8-二氮杂二环[4.3.0]壬烷的拆分
    • WO0076996A2
    • 2000-12-21
    • PCT/EP0005116
    • 2000-06-05
    • BAYER AGFEY PETER
    • FEY PETER
    • C07D471/04C07H9/04
    • C07D471/04C07H9/04
    • The invention relates to a method for the enantiomer separation of cis-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane (also described below as cis-6-benzyl-5,7-dioxooctahydropyrrolo[3,4-b]pyridine or dioxopyrrolopiperidine). The invention also relates to a method for producing (1S, 6R)- and (1R, 6S)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane using the above method. The invention further relates to the (-)-2,3:4,6-di-O-isopropylidene-2-keto-L- gulonic acid salts of (1S, 6R)- and (1R, 6S)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane and to a method for producing the same. Finally, the invention relates to a method for the enantiomer enrichment of (1S, 6R)-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]-nonane.
    • 本发明涉及一种用于顺式-8-苄基-7,9-二氧代-2,8-二氮杂二环[4.3.0]的对映异构体的分离壬烷(在下文中也被称作顺式-6-苄基-5,7- dioxooctahydropyrrolo [3- ,4-b]吡啶或下文Dioxopyrrolopiperidin)。 在另一个方面,本发明涉及一种用于(1S,6R)的制备 - 和(1R,6S)-8-苄基-7,9-二氧代-2,8-二氮杂二环[4.3.0]壬烷,使用上述 流程。 此外,本发明涉及( - ) - 2,3:4,6-二-O-异丙叉基-2-酮-L-gulonsäuresalze(1S,6R) - 和(1R,6S)-8-苄基-7-, 9二氧代-2,8-二氮杂二环[4.3.0]壬烷和它们的制备过程。 此外,本发明涉及一种用于对映体富集的处理(1S,6R)-8-苄基-7,9-二氧代-2,8-二氮杂二环[4.3.0]壬烷。
    • 7. 发明申请
    • NOVEL HIGH ENANTIO-SELECTIVE PROCESS FOR PRODUCING PURE ENANTIOMERIC CYCLOPENTANE AND CYCLOPENTENE-'beta'-AMINO ACIDS
    • 新型高对映选择性方法用于生产对映体纯环戊烷和-PENTEN-β-氨基酸
    • WO1995019337A1
    • 1995-07-20
    • PCT/EP1995000059
    • 1995-01-09
    • BAYER AKTIENGESELLSCHAFTMITTENDORF, JoachimAROLD, HermannFEY, PeterMATZKE, MichaelMILITZER, Hans-ChristianMOHRS, Klaus-Helmut
    • BAYER AKTIENGESELLSCHAFT
    • C07C227/32
    • C07C229/48C07C69/74C07C227/32C07C271/24C07C2601/08Y02P20/55
    • The present invention relates to a high enantio-selective process for producing pure enantiomeric cyclopentane and cyclopentene- beta -amino acids of the general formula (I) in which A and L, A and D or E and L, D and E, R , R , T and R have the meanings given in the description. In the process, meso-dicarboxylic acid anhydride is first converted into the enantiomer-free dicarboxylic acid mono-ester via the intermediate, enantiomer-free salt stage by asymmetrical alcoholysis with alcohols and in the presence of equimolar quantities of a chiral amine base in enantiomer-free form, in inert solvents, and then the enantiomer-free amides are produced after NH3 activation, the ester group is separated out in a further step and finally a Hofmann transposition is performed with alkaline or alkaline earth hypochlorites in an aqueous alkaline or alkaline earth hydroxide solution, in solution the free amine function is first blocked with a typical amino-protective group and, after the protected compounds have been isolated in normal conditions, they are separated out by the usual methods, retaining the pure enantiomer.
    • 本发明涉及一种用于对映体纯环戊烷和-penten-的β的制备高对映选择性方法氨基的通式(I)的酸,其中A和L,A和D或E和L,D和E,R <2>, [R <3>,T和R <1>具有说明书中给出的含义。 该方法的特征在于,内消旋 - 二羧酸酐第一通过不对称醇解用的醇并在对映体纯形式,手性胺碱,在惰性溶剂中的等摩尔量的本的存在下转化,经由中间,对映体纯Salztufe到对映体纯的二羧酸单酯,然后激活 NH 3,对映异构纯的酰胺制备,在进一步的步骤中裂解掉酯基,最后用,并经过典型氨基封端从而隔离的保护的化合物的最初进行霍夫曼重排用碱金属或含水的碱金属或碱土金属氢氧化物碱土金属次氯酸盐,在溶液中的游离胺官能团 裂解以常规条件,包括接收到相应纯对映体的,通过常规的方法。