Diaryl phosphine compounds
    75.
    发明授权
    Diaryl phosphine compounds 有权
    二芳基膦化合物

    公开(公告)号:US08871916B2

    公开(公告)日:2014-10-28

    申请号:US13715842

    申请日:2012-12-14

    摘要: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diazo-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compounds and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.

    摘要翻译: 制备重氮化合物,其重氮盐和这些化合物的其它保护形式的方法。 重氮化合物是通过将载有反应性羰基的叔膦试剂与叠氮化物反应来制备的。 反应也可以产生酰基三氮烯,其可以热转化或加入碱形成重氮化合物,或者可以分离酰基三氮烯。 该方法对于携带一个或多个吸电子基团的叠氮化物转化为重氮化合物是特别有用的。 该方法可以在温和条件下在水性介质中进行,特别适用于在生理条件下将叠氮基糖转化为重氮化合物和重氮盐。 提供了叔膦试剂,特别是水溶性试剂,以及制备试剂的前体。

    Selective and Specific Preparation of Discrete Peg Compounds
    77.
    发明申请
    Selective and Specific Preparation of Discrete Peg Compounds 有权
    离散聚合物的选择性和特异性制备

    公开(公告)号:US20110124844A1

    公开(公告)日:2011-05-26

    申请号:US13014789

    申请日:2011-01-27

    摘要: Aspects of the present invention are directed to novel methods for making discrete polyethylene compounds selectively and specifically to a predetermined number of ethylene oxide units. Methods which can be used to build up larger dPEG compounds (a) containing a wider range of utility to make useful homo- and heterofunctional and branched species, and (b) under reaction configurations and conditions that are milder, more efficient, more diverse in terms of incorporating useful functionality, more controllable, and more versatile then any conventional method reported in the art to date. In addition, the embodiments of the invention allow for processes that allow for significantly improving the ability to purify the intermediates or final product mixtures, making these methods useful for commerial manufacturing dPEGs. Protecting groups and functional groups can be designed to make purification at large scale a practical reality. The novel dPEG products form the compositional and material basis for making other novel compounds of valuable application in the fields of diagnostics and therapeutics, amongst others.

    摘要翻译: 本发明的方面涉及选择性地且具体地制备离散聚乙烯化合物至预定数量的环氧乙烷单元的新方法。 可用于建立较大的dPEG化合物的方法(a),其具有更广泛的用途以实现有用的同功和异功能和支链物质,以及(b)在温和,更有效,更多样化的反应配置和条件下 迄今为止本领域所报道的任何常规方法,结合有用的功能,更可控和更通用的术语。 此外,本发明的实施方案允许允许显着提高纯化中间体或最终产物混合物的能力的方法,使得这些方法对于商业制造dPEG有用。 保护群体和功能团体可以设计成大规模净化实际的现实。 新型dPEG产品形成了其他新型化合物在诊断和治疗领域的有价值应用的组成和物质基础。