アミン類の製造方法
    3.
    发明申请
    アミン類の製造方法 审中-公开
    生产氨基酸的方法

    公开(公告)号:WO2005070875A1

    公开(公告)日:2005-08-04

    申请号:PCT/JP2005/000962

    申请日:2005-01-26

    IPC分类号: C07C221/00

    摘要: A process for the production of amines which is characterized by reacting an imine with a nucleophilic compound (except trialkylsilyl vinyl ethers) in the presence of a phosphoric acid derivative represented by the general formula (1): (1) (wherein A is a spacer; X and X are each independently a divalent nonmetal atom or a divalent nonmetal atomic group; and Y is oxygen or sulfur). The invention provides a process by which amines (particularly optically active amines) useful as intermediates of drugs, agricultural chemicals, or the like can be produced without special post-treatment in high yield at high optical purity; and phosphoric acid derivatives (particularly optically active phosphoric acid derivatives) useful in the production of the amines.

    摘要翻译: 一种制备胺的方法,其特征在于在通式(1)表示的磷酸衍生物存在下使亚胺与亲核化合物(三烷基甲硅烷基乙烯基醚除外)反应:(1)(其中A 1 是间隔基; X 1和X 2各自独立地为二价非金属原子或二价非金属原子团; Y 1为氧或硫)。 本发明提供了一种可以在高光学纯度下以高产率而不用特殊后处理而用作药物,农药等中间体的胺(特别是光学活性胺)的方法。 和可用于制备胺的磷酸衍生物(特别是光学活性磷酸衍生物)。

    CONTINUOUS PRODUCTION AND REACTION OF A DIAZO COMPOUND
    4.
    发明申请
    CONTINUOUS PRODUCTION AND REACTION OF A DIAZO COMPOUND 审中-公开
    连氮化合物的连续生产和反应

    公开(公告)号:WO2012059485A2

    公开(公告)日:2012-05-10

    申请号:PCT/EP2011069186

    申请日:2011-11-01

    摘要: A process for producing a reaction product of a diazo compound, which process comprises: a. continuously supplying to a first reactor a precursor of a diazo compound; a water-miscible solvent; a base and water; b. mixing the precursor of a diazo compound; the water-miscible solvent; the base and water to generate a diazo compound; c. continuously removing from the first reactor, through a hydrophobic membrane, into a second reactor the formed diazo compound; d. continuously removing from the first reactor all reaction products that have not passed into the second reactor; e. continuously supplying to the second reactor a substrate in a non-water-miscible solvent; f. mixing the above components to generate a reaction product of a diazo compound; and g. continuously removing from the second reactor the non-water-miscible solvent and the reaction product of the diazo compound, and apparatus suitable for carrying out such a process.

    摘要翻译: 一种制备重氮化合物反应产物的方法,该方法包括:a。 向第一反应器连续供应重氮化合物的前体; 一种与水混溶的溶剂; 一个基地和水; 湾 混合重氮化合物的前体; 与水混溶的溶剂; 该碱和水生成重氮化合物; C。 连续地从第一反应器中通过疏水膜除去形成的重氮化合物到第二反应器中; d。 不断从第一反应器中取出所有未通入第二反应器的反应产物; 即 在非水混溶性溶剂中向第二反应器连续供应基材; F。 混合上述组分以产生重氮化合物的反应产物; 和g。 从第二反应器中连续地除去不与水混溶的溶剂和重氮化合物的反应产物,以及适于实施这种方法的设备。

    DIPEPTIDYL PEPTIDASE-I, CLONING IT, AND THERAPEUTIC AGENTS CONTAINING INHIBITORS THEREOF
    6.
    发明申请
    DIPEPTIDYL PEPTIDASE-I, CLONING IT, AND THERAPEUTIC AGENTS CONTAINING INHIBITORS THEREOF 审中-公开
    DIPEPTIDYL PEPTIDASE-I,克隆及其含有抑制剂的治疗剂

    公开(公告)号:WO1993024634A1

    公开(公告)日:1993-12-09

    申请号:PCT/US1993005093

    申请日:1993-05-28

    IPC分类号: C12N15/57

    摘要: Therapeutic agents and methods for the treatment of immunologically mediated diseases and malignancies of myeloid cell or lymphoid cell origin. These particular methods utilize the characterization of particular activation mechanisms important to the progression of these pathologies in humans. Selective inhibition of cell types responsible for precipitating these disorders in humans are provided with therapeutic agents which include peptides capable of inhibiting dipeptidyl peptidase-I activation of proenzymes present primarily in cytotoxic T-cells and myeloid cells, such as Gly-Phe-CHN2. Antisense oligonucleotides are also characterized which are specific for human dipeptidyl peptidase-I gene which may be used in the treatment of the described disorders.

    摘要翻译: 用于治疗免疫介导的疾病和骨髓细胞或淋巴细胞起源的恶性肿瘤的治疗剂和方法。 这些特定的方法利用对人类这些病理进展重要的特定活化机制的表征。 提供了负责沉淀人类这些疾病的细胞类型的选择性抑制,其包括能够抑制主要存在于细胞毒性T细胞和骨髓细胞如Gly-Phe-CHN2中的酶的二肽基肽酶-I活化的肽。 还表征了反义寡核苷酸,其可用于治疗所述疾病的人二肽基肽酶-I基因。

    CHEMICALLY INERT MOLECULAR TAGS
    7.
    发明申请
    CHEMICALLY INERT MOLECULAR TAGS 审中-公开
    化学分子标记

    公开(公告)号:WO2003093823A2

    公开(公告)日:2003-11-13

    申请号:PCT/US2003/012325

    申请日:2003-04-22

    IPC分类号: G01N33/543

    摘要: A method for identifying a solid support in combinatorial synthesis or determining the structure of a compound in combinatorial synthesis. The method involves attaching, detaching and identifying at least one tag by detaching the tag from the solid support and reacting the detached tag with a fluoroalkanoyl acid or its alcohol-reactive equivalent. A preferred linker/tag is of formula -C(=O)C6H3(OCH3)-OR1 in which R1 is C13 to C33 alkane or ether.

    摘要翻译: 用于在组合合成中鉴定固体支持物或确定组合合成中化合物的结构的方法。 该方法包括通过从固体支持物上分离标签并使分离的标签与氟烷酰基酸或其醇反应性等价物反应来附接,分离和鉴定至少一个标签。 优选的接头/标签具有式-C(= O)C 6 H 3(OCH 3)-OR 1,其中R 1是C 13至C 33烷烃或醚。

    PROCESS FOR PRODUCING DIAZOMETHANE DERIVATIVE
    10.
    发明申请
    PROCESS FOR PRODUCING DIAZOMETHANE DERIVATIVE 审中-公开
    生产二唑衍生物的方法

    公开(公告)号:WO1995016666A1

    公开(公告)日:1995-06-22

    申请号:PCT/JP1994002124

    申请日:1994-12-16

    IPC分类号: C07C245/16

    CPC分类号: C07C245/14

    摘要: A process for producing a diazomethane derivative by oxidizing a hydrazone derivative in a two-phase system containing: a) an aqueous solution of a mixture of a caustic alkali and an alkali metal hypochlorite in respective concentrations of 4-14 w/w % and 3-10 w/w % based on the total weight of the solution; b) a hydrophobic organic solvent; c) an inorganic iodine compound, and d) a phase-transfer catalyst.

    摘要翻译: 通过在两相体系中氧化腙衍生物来制备重氮甲烷衍生物的方法,其包含:a)苛性碱和碱金属次氯酸盐的混合物的水溶液,其浓度分别为4-14w / w%和3 -10w / w%,基于溶液的总重量; b)疏水性有机溶剂; c)无机碘化合物,和d)相转移催化剂。