PROCESS FOR THE PREPARATION OF 4,5-DIAMINO SHIKIMICACID
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF 4,5-DIAMINO SHIKIMICACID 审中-公开
    制备4,5-DIAMINO SHIKIMICICID的方法

    公开(公告)号:WO2006024436A1

    公开(公告)日:2006-03-09

    申请号:PCT/EP2005/009121

    申请日:2005-08-24

    摘要: The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula (I) and pharmaceutically acceptable addition salts thereof wherein R 1 , R 1’ are independent of each other H or alkyl, R 2 is an alkyl and R 3 , R 4 are independent of each other H or an alkanoyl, with the proviso that not to both R 3 and R 4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5­-amino-4-acetylamino-3- (1-ethyl-propoxy)-cyclohex-l-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.

    摘要翻译: 本发明涉及制备式(I)的4,5-二氨基莽虫酸衍生物及其药学上可接受的加成盐的方法,其中R

    PRODUCTION OF ALKYL 6-AMINOCAPROATE
    4.
    发明申请
    PRODUCTION OF ALKYL 6-AMINOCAPROATE 审中-公开
    产品6-AMINOCAPROATE ALKYL

    公开(公告)号:WO02040452A2

    公开(公告)日:2002-05-23

    申请号:PCT/US2001/047424

    申请日:2001-11-05

    CPC分类号: C07C227/12 C07C229/08

    摘要: A process for making alkyl 6-aminocaproate by hydroformylating 3-pentenenitrile to produce 3-, 4-, and 5-formylvaleronitrile (FVN mixture), converting the FVN mixture to alkyl 3-, 4-, and 5-cyanovalerate by either oxidative esterification of the FVN mixture or oxidation of the FVN mixture followed by esterification; isolating alkyl 5-cyanovalerate; and hydrogenating the alkyl 5-cyanovalerate to produce alkyl 6-aminocaproate. The resulting alkyl 6-aminocaproate can be cyclized to produce caprolactam.

    摘要翻译: 本发明涉及一种通过3-戊烯腈的加氢甲酰化制备烷基的6-氨基己的过程在3-,以产生3-,4-,和5- formylvaleronitrile(FVN混合物),由FVN混合物的转化,4-,和 烷基-5-氰基戊或者由FVN混合物的氧化酯化,或通过由5-氰基戊分离和烷基由5-氰基戊烷基的氢化以制造氧化FVN混合物中,随后酯化, 6-氨基己酸烷基酯。 得到的6-氨基己酸烷基酯可以环化生成己内酰胺。

    AMINE DERIVATIVE FIXED TO RESIN AND METHOD FOR SYNTHESIZING beta -AMINOCARBONYL COMPOUND IN A SOLID PHASE
    7.
    发明申请
    AMINE DERIVATIVE FIXED TO RESIN AND METHOD FOR SYNTHESIZING beta -AMINOCARBONYL COMPOUND IN A SOLID PHASE 审中-公开
    固定于树脂上的胺衍生物和在固相中合成β-亚氨基羰基化合物的方法

    公开(公告)号:WO99046239A1

    公开(公告)日:1999-09-16

    申请号:PCT/JP1999/001221

    申请日:1999-03-12

    摘要: An imine fixed to a resin characterized in that it is represented by the following formula: P-Q-N=CH-R wherein P represents a main chain of a polymer constituting the resin, Q represents a hydrocarbon side chain optionally substituted with a substituent which may be bonded via a heteroatom and R represents an optionally substituted hydrocarbon group or a heterocyclic group, and a beta -aminocarbonyl compound fixed to a resin represented by formula (II) are provided. The beta -aminocarbonyl compound fixed to a resin is a beta -aminocarbonyl compound being handled in a solid form. An amine fixed to a resin which is a key compound for a solid state synthesis of this type and represented by the following formula: P-Q1-O-Q2-NH2, wherein Q1 and Q2 are each a hydrocarbon chain selected from among an arylene group, an alkylarylene group and an arylenealkylene group, is also provided, which allows the synthesis of beta -aminocarbonyl compound by application of an iminoaldol reaction in a solid phase.

    摘要翻译: 固定在树脂上的亚胺,其特征在于其由下式表示:PQN = CH-R其中P表示构成树脂的聚合物的主链,Q表示任选被可被键合的取代基取代的烃侧链 通过杂原子和R表示任选取代的烃基或杂环基,并且提供固定在由式(II)表示的树脂上的β-氨基羰基化合物。 固定在树脂上的β-氨基羰基化合物是以固体形式处理的β-氨基羰基化合物。 固定在树脂上的胺,它是这种类型的固态合成的关键化合物,由下式表示:P-Q1-O-Q2-NH2,其中Q1和Q2各自为选自亚芳基 基团,亚烷基亚芳基和亚芳基亚烷基,其允许通过在固相中应用亚氨基醇反应合成β-氨基羰基化合物。