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    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE
    4.
    发明公开
    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN 2-ARYLPIPERAZINDERIVATS

    公开(公告)号：EP2119709A1

    公开(公告)日：2009-11-18

    申请号：EP08710788.4

    申请日：2008-02-05

    申请人： Kaneka Corporation

    发明人： OHNUKI, Masatoshi ,  NISHIYAMA, Akira ,  MITSUDA, Masaru

    IPC分类号： C07D241/04 ,  C07B53/00

    CPC分类号： C07B53/00 ,  C07D241/04

    摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.

    摘要翻译： 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物制备的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物。 特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

    PROCESS FOR PRODUCING CYSTEINE DERIVATIVES
    8.
    发明公开
    PROCESS FOR PRODUCING CYSTEINE DERIVATIVES 失效
    VERFAHREN ZUR HERSTELLUNG VON CYSTEIN DERIVATEN

    公开(公告)号：EP0897911A1

    公开(公告)日：1999-02-24

    申请号：EP98900354.6

    申请日：1998-01-14

    申请人： KANEKA CORPORATION

    发明人： KONDO, Takeshi ,  NISHIYAMA, Akira ,  UEYAMA, Noboru ,  MURAO, Hiroshi ,  MANABE, Hajime ,  UEDA, Yasuyoshi

    IPC分类号： C07C323/58 ,  C07C319/14 ,  B01J31/02

    CPC分类号： C07C319/14 ,  C07B2200/07 ,  Y02P20/55 ,  C07C323/58 ,  C07C323/59

    摘要： This invention relates to a method comprising reacting an amino acid derivative of the following general formula (I):
    (wherein R 1 represents an amino-protective group; R 0 represents hydrogen or, taken together with R 1 , represents an amino-protecting group; R 2 represents a carboxy-protecting group; X represents a leaving group) with a thiol compound of the following general formula (II):

            R 3 SH     (II)

    (wherein R 3 represents an alkyl group of 1 to 7 carbon atoms, an aryl group of 6 to 10 carbon atoms, or an aralkyl group of 7 to 10 carbon atoms) to give a cysteine derivative of the following general formula (III):
    (wherein R 0 , R 1 , R 2 , and R 3 are as defined above), wherein the reaction is conducted in the presence of a base and water in an organic reaction solvent.

    摘要翻译： 本发明涉及使下列通式（I）的氨基酸衍生物：其中R 1表示氨基保护基，R 0表示氢或与R' 1表示氨基保护基; R 2表示羧基保护基; X表示离去基团）与下列通式（II）的硫醇化合物反应：R 3 SH（其中R 3 >表示1〜7个碳原子的烷基，6〜10个碳原子的芳基或7〜10个碳原子的芳烷基），得到下述通式（III）的半胱氨酸衍生物： （其中R 0，R 1，R 2和R 3如上所定义），其中反应在碱和水的存在下在有机反应溶剂中进行。

    METHOD FOR PRODUCING LONG-CHAIN PEPTIDE
    9.
    发明公开
    METHOD FOR PRODUCING LONG-CHAIN PEPTIDE 审中-公开

    公开(公告)号：EP3778620A1

    公开(公告)日：2021-02-17

    申请号：EP19777967.1

    申请日：2019-01-08

    申请人： KANEKA CORPORATION

    发明人： MURATA, Takahiko ,  YAMAMOTO, Shohei ,  NISHIYAMA, Akira

    IPC分类号： C07K1/02 ,  C07K1/06

    摘要： The objective of the present invention is to provide a method for efficiently producing a long-chain peptide which method is suitable even for an industrial large scale production. The method for producing a long-chain peptide according to the present invention is characterized in comprising a step to deprotect an N-terminal site protected with BOC of a raw material peptide fragment with using a sulfonic acid compound, a step to selectively deprotect a C-terminal site protected with ONBn of a raw material peptide, and a step to condensate the obtained peptide fragment having the deprotected N-terminal site and the obtained peptide fragment having the deprotected C-terminal site in a liquid phase condition.

    ORGANIC COMPOUND PRODUCTION METHOD
    10.
    发明公开
    ORGANIC COMPOUND PRODUCTION METHOD 审中-公开

    公开(公告)号：EP3680235A1

    公开(公告)日：2020-07-15

    申请号：EP18853393.9

    申请日：2018-08-07

    申请人： Kaneka Corporation

    发明人： YASUKOUCHI, Hiroaki ,  NISHIYAMA, Akira ,  MACHIDA, Koji

    IPC分类号： C07D217/06

    摘要： The purpose of the present invention is to further enhance a product yield when a phosgene alternative reagent is used in a flow reactor. A process for producing an organic compound using a flow reactor for a first reaction in which a raw material liquid A and a raw material liquid B are mixed, and reacted in a reactor unit, and a flow reactor for a second reaction in which a first reaction solution discharged from the flow reactor for the first reaction and a raw material liquid C are mixed, and reacted in a reactor unit, wherein the raw material liquid A is a solution in which triphosgene and/or diphosgene is dissolved, wherein the raw material liquid B is a nitrogen-containing organic compound or a solution of the nitrogen-containing organic compound, wherein the raw material liquid C is a reaction substrate having functional group capable of reacting with phosgene, the functional group being selected from the group consisting of an amino group, an amido group, and -OC(=O)NH 2 , or a solution containing the reaction substrate, and wherein a product of the first reaction is phosgene.