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    One pot synthesis of tetrazole derivatives of sirolimus
    44.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2014200017B2

    公开(公告)日：2016-06-09

    申请号：AU2014200017

    申请日：2014-01-03

    Applicant: ABBOTT LAB

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

    IPC: C07D498/18 ,  A61K31/395

    Abstract: ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 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.

    One pot synthesis of tetrazole derivatives of sirolimus
    45.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2014200017A1

    公开(公告)日：2014-01-23

    申请号：AU2014200017

    申请日：2014-01-03

    Applicant: ABBOTT LAB

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

    IPC: C07D498/18 ,  A61K31/395

    Abstract: ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 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.

    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    47.
    发明专利
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 未知

    公开(公告)号：CA2997700A1

    公开(公告)日：2007-08-23

    申请号：CA2997700

    申请日：2006-12-12

    Applicant: ABBOTT LAB

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

    IPC: 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.

    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    48.
    发明专利
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 未知

    公开(公告)号：CA2631971A1

    公开(公告)日：2007-08-23

    申请号：CA2631971

    申请日：2006-12-12

    Applicant: ABBOTT LAB

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

    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 o ne embodiment, dried rapamycin is dissolved in isopropylacetate . After cooling and 2,6-Lutidine addition, triflic anhydride is slowly added at -30~ C. Salt s 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/heptan e as eluant. The product is collected, concentrated, and purified using an acetone/heptane column. The product-containing fractions are concentrated. T he product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene, and the soluti on 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.

    One pot synthesis of tetrazole derivatives of sirolimus
    49.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2006338175A1

    公开(公告)日：2007-08-23

    申请号：AU2006338175

    申请日：2006-12-12

    Applicant: ABBOTT LAB

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

    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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