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    One pot synthesis of tetrazole derivatives of sirolimus
    13.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2016203198A1

    公开(公告)日：2016-06-09

    申请号：AU2016203198

    申请日：2016-05-17

    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 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
    14.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：ZA200804209B

    公开(公告)日：2010-08-25

    申请号：ZA200804209

    申请日：2006-12-12

    Applicant: ABBOTT LAB

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

    IPC: A61K20060101 ,  C07D20060101

    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
    16.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：AU2006338175A2

    公开(公告)日：2009-03-12

    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.

    SINTESIS EN UN SOLO RECIPIENTE DE DERIVADOS TETRAZOLICOS DE RAPAMICINA(SIROLIMUS) Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN.
    17.
    发明专利
    SINTESIS EN UN SOLO RECIPIENTE DE DERIVADOS TETRAZOLICOS DE RAPAMICINA(SIROLIMUS) Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. 未知

    公开(公告)号：AR058545A1

    公开(公告)日：2008-02-13

    申请号：ARP060105535

    申请日：2006-12-14

    Applicant: ABBOTT LAB

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

    IPC: C07D498/18 ,  C07D249/06 ,  A61K31/395 ,  A61P35/00 ,  A61P31/10 ,  A61P37/06 ,  C07D311/00 ,  C07D273/00 ,  C07D221/00

    Abstract: Reivindicacion 1: Un método para preparar una molécula de formula (1) caracterizado porque comprende (a) hacer reaccionar una molécula de formula (2) con anhídrido tríflico, para producir una molécula de formula (3) y (b) hacer reaccionar la molécula de formula (3) con una molécula de formula (4) donde R1 se selecciona del grupo que consiste en =O(H, H) y (H, OH); R2 y R5 se seleccionan independientemente del grupo que consiste en H, -C(=O)R6, -C(=O)OR6, -C(=O)NHR6 y -C(=S)OR6; R3 se selecciona del grupo que consiste en =O y OR5; o R2 y R3 pueden tomarse juntos para formar una porcion de formula A-C(R7)(R8)-O-B, donde A es un enlace a un O unido al C 28 y B está unido al C 28, como se definio con anterioridad; R4 se selecciona del grupo que consiste en H y alquilo C1-4; R6 se selecciona del grupo que consiste en alquilo C1-10, cicloalquilo C3-6, grupos arilo y grupos heterocíclicos; R7 y R8 se seleccionan independientemente del grupo que consiste en H, alquilo C1-6, o R7 y R8 tomados juntos son =O; R9 y R10 se seleccionan independientemente del grupo que consiste en H, alquenilo, alquenilcicloalquenilo, alquenilcicloalquilo, alquilo, alquilcicloalquenilo, alquilcicloalquilo, alquinilo, aralquilo, arilo, cicloalquenilo, cicloalquilo, cicloalquilalquilo, cicloalquilcicloalquilo, cicloalquenilalquilo, heterociclilo, aza, amida, amonio, oxa, tia, sulfonilo, sulfinilo, sulfonamida, fosforilo, fosfinilo, fosfino, fosfonio, ceto, éster, alcohol, carbamato, urea, tiocarbonilo, boratos, boranos, boraza, sililo, siloxilo, silaza, y combinaciones de estos. Reivindicacion 2: El método de la reivindicacion 1, caracterizado porque se realiza en un solo recipiente.

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