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    One pot synthesis of tetrazole derivative of sirolimus
    1.
    发明专利
    One pot synthesis of tetrazole derivative of sirolimus 审中-公开
    SIROLIMUS四唑衍生物的一个合成

    公开(公告)号：JP2013032368A

    公开(公告)日：2013-02-14

    申请号：JP2012212779

    申请日：2012-09-26

    Applicant: Abbott Lab ,  アボット ラボラトリーズ

    Inventor： DHAON MADHUP ,  HSIAO CHU-NUNG ,  PATEL SUBHASH ,  BONK PETER ,  CHEMBURKAR SANJAY ,  CHEN YONG

    IPC: A61K31/436 ,  A61K47/10 ,  A61K47/22 ,  A61P19/02 ,  A61P29/00 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06 ,  C07C39/06 ,  C07C43/23 ,  C07C57/15 ,  C07C69/84

    CPC classification number: C07D498/18

    Abstract: PROBLEM TO BE SOLVED: To provide a single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale.SOLUTION: Dried rapamycin is dissolved in isopropylacetate. After cooling and 2,6-lutidine addition, triflic anhydride is slowly added at -30°C. Salts are removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine is added. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as an eluant. The product is collected, concentrated, and purified using an acetone/heptane column. The product-containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone and treated with butylated-hydroxy toluene, and the solution is concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.

    Abstract translation: 要解决的问题：提供一步一步一锅法以大规模获得唑他罗莫斯和其他雷帕霉素衍生物。 解决方案：将干雷帕霉素溶于乙酸异丙酯。 冷却后加入2,6-二甲基吡啶，在-30℃下缓慢加入三氟甲磺酸酐。 通过过滤除去盐。 加入四唑，然后加入叔 - 碱二异丙基乙胺。 在室温下孵育后，将产物浓缩并通过硅胶柱纯化，使用THF /庚烷作为洗脱剂。 使用丙酮/庚烷柱收集，浓缩和纯化产物。 将含产物的级分浓缩。 将产物溶于t-BME中并用庚烷沉淀。 将固体溶解在丙酮中并用丁基化羟基甲苯处理，浓缩溶液。 用丙酮重复该过程两次以除去溶剂。 在干燥前加入至少一种稳定剂，例如0.5％的BHT。 版权所有（C）2013，JPO＆INPIT

    One-pot synthesis of tetrazole derivatives of sirolimus
    2.
    发明专利
    One-pot synthesis of tetrazole derivatives of sirolimus 审中-公开
    SIROLIMUS四唑衍生物的一步合成

    公开(公告)号：JP2013032367A

    公开(公告)日：2013-02-14

    申请号：JP2012212775

    申请日：2012-09-26

    Applicant: Abbott Lab ,  アボット ラボラトリーズ

    Inventor： DHAON MADHUP ,  HSIAO CHU-NUNG ,  PATEL SUBHASH ,  BONK PETER ,  CHEMBURKAR SANJAY ,  CHEN YONG

    IPC: C07D498/18 ,  A61K31/436 ,  A61P19/02 ,  A61P29/00 ,  A61P31/10 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06

    CPC classification number: C07D498/18

    Abstract: PROBLEM TO BE SOLVED: To provide a one-pot synthesizing process to obtain zotarolimus and other rapamycin derivatives on large scale.SOLUTION: A dried rapamycin is dissolved in isopropyl acetate. The solution is cooled, and 2,6-Lutidine is added, followed by slowly adding trifluoromethanesulfonic anhydride at -30°C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine is added. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.

    Abstract translation: 待解决的问题：提供一锅合成方法以大规模获得唑他罗莫司和其他雷帕霉素衍生物。 解决方案：将干燥的雷帕霉素溶解在乙酸异丙酯中。 将溶液冷却，加入2,6-二甲基吡啶，然后在-30℃下缓慢加入三氟甲磺酸酐。 然后通过过滤除去盐。 加入四唑，然后加入叔 - 碱二异丙基乙胺。 在室温下孵育后，将产物浓缩并通过硅胶柱纯化，使用THF /庚烷作为洗脱剂。 收集含有产物的级分，浓缩并再次使用丙酮/庚烷柱纯化。 将含产物的级分浓缩。 将产物溶于t-BME中并用庚烷沉淀。 将固体溶解在丙酮中，用丁基化羟基甲苯（BHT）处理，浓缩溶液。 用丙酮重复该过程两次以除去溶剂。 在干燥前加入至少一种稳定剂，例如0.5％的BHT。 版权所有（C）2013，JPO＆INPIT

    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    3.
    发明申请
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 审中-公开
    一锅法合成四螺旋四唑衍生物

    公开(公告)号：WO2007094886A3

    公开(公告)日：2007-11-29

    申请号：PCT/US2006061909

    申请日：2006-12-12

    Applicant: ABBOTT LAB ,  DHAON MADHUP ,  HSIAO CHU-NUNG ,  PATEL SUBHASH ,  BONK PETER ,  CHEMBURKAR SANJAY ,  CHEN YONG

    Inventor： DHAON MADHUP ,  HSIAO CHU-NUNG ,  PATEL SUBHASH ,  BONK PETER ,  CHEMBURKAR SANJAY ,  CHEN YONG

    IPC: C07D498/18 ,  A61K31/395

    CPC classification number: C07D498/18

    Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale that improves currently available syntheses. In one embodiment, dried rapamycin is dissolved in isopropylacetate . After cooling and 2,6-Lutidine addition, triflic anhydride is slowly added at -30° C. Salts are removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine is added. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The product is collected, concentrated, and purified using an acetone/heptane column. The product-containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene, and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.

    Abstract translation: 大规模获得zotarolimus和其他雷帕霉素衍生物的单步一锅法工艺，改进了目前可用的合成方法。 在一个实施方案中，将干燥的雷帕霉素溶解在乙酸异丙酯中。 冷却并加入2,6-二甲基吡啶后，在-30℃缓慢加入三氟甲磺酸酐。过滤除去盐。 加入四唑，然后加入叔丁基二异丙基乙胺。 在室温下温育后，将产物浓缩并通过硅胶柱使用THF /庚烷作为洗脱液进行纯化。 收集产物，浓缩并使用丙酮/庚烷柱纯化。 含产物的级分被浓缩。 将产物溶解在t-BME中并用庚烷沉淀。 将固体溶于丙酮中，用丁基化羟基甲苯处理，浓缩溶液。 该过程用丙酮重复两次以除去溶剂。 在干燥前加入至少一种稳定剂，例如0.5％的BHT。

    One pot synthesis of tetrazole derivatives of sirolimus
    6.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2006338175B2

    公开(公告)日：2013-10-03

    申请号：AU2006338175

    申请日：2006-12-12

    Applicant: ABBOTT LAB

    Inventor： CHEMBURKAR SANJAY ,  HSIAO CHU-NUNG ,  PATEL SUBHASH ,  BONK PETER ,  DHAON MADHUP ,  CHEN YOUNG

    IPC: C07D498/18 ,  A61K31/395

    Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale that improves currently available syntheses. In one embodiment, dried rapamycin is dissolved in isopropylacetate . After cooling and 2,6-Lutidine addition, triflic anhydride is slowly added at -30° C. Salts are removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine is added. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The product is collected, concentrated, and purified using an acetone/heptane column. The product-containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene, and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.

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