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Radio-iodinated tyrosine derivs. of oestradiol oxime cpds. - useful as reagents for radioimmunoassay of oestradiol

机译:放射性碘的酪氨酸衍生物。雌二醇肟cpds。 -用作雌二醇放射免疫分析的试剂

摘要

Oestradiol derivs. of formula (I) are new. (where R = tyrosine residue, tyrosine 1-6 C alkyl ester residue, radioiodinated tyrosine residue, or radioiodinated tyrosine 1-6 C alkyl residue). Cpds. (I) in which R is a radioiodinated tyrosine or tyrosine alkyl ester residue are useful as reagents for the radioimmunoassay of oestradiol; in a highly specific manner, they form complexes with oestradiol antibodies. Other cpds. (I) are useful as intermediates for the radio-iodinated cpds. A procedure for carrying out a radio-immunoassay with the new cpds. is described in the specification. Specific cpds. (I) include that in which R is a tyrosine methyl ester residue. In an example, this is prepd. by reacting 6-(carboxymthoxyimino)-oestradiol with isobutyl chlorocarbonate in dioxan in the presence of tributylamine and reacting the resulting mixed anhydride with L-tyrosine methyl ester. Reaction of the product with Na125I in the presence of chloramine T and hydrolysis with NAOH gives (I) in which R is a 125I-tyrosine residue.
机译:雌二醇衍生。式(I)的化学式是新的。 (其中R =酪氨酸残基,酪氨酸1-6C烷基酯残基,放射性碘化酪氨酸残基或放射性碘化酪氨酸1-6C烷基残基)。 Cpds。 (I)其中R是放射性碘化的酪氨酸或酪氨酸烷基酯残基用作雌二醇的放射免疫测定的试剂;它们以高度特异性的方式与雌二醇抗体形成复合物。其他cpds。 (I)可用作放射性碘的cpds的中间体。用新的cpds进行放射免疫测定的程序。在规范中进行了描述。特定的cpds。 (I)包括其中R是酪氨酸甲酯残基的残基。在一个示例中,这是准备的。在三丁胺的存在下,使6-(羧基甲氧基亚氨基)-雌二醇与氯代碳酸异丁酯在二恶烷中反应,并使所得的混合酸酐与L-酪氨酸甲酯反应。产物在氯胺T存在下与Na125I反应,并与NAOH水解,得到(I),其中R是125I-酪氨酸残基。

著录项

  • 公开/公告号FR2393009A1

    专利类型

  • 公开/公告日1978-12-29

    原文格式PDF

  • 申请/专利权人 DAIICHI RADIOISOTOPE LABORATORIE;

    申请/专利号FR19780010110

  • 发明设计人

    申请日1978-04-05

  • 分类号C07J1/00;G01N33/16;G21H5/02;

  • 国家 FR

  • 入库时间 2022-08-22 19:35:01

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