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    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    31.
    发明专利
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 未知

    公开(公告)号：CA2631971C

    公开(公告)日：2016-10-04

    申请号：CA2631971

    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 ,  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.

    One pot synthesis of tetrazole derivatives of sirolimus
    32.
    发明专利
    One pot synthesis of tetrazole derivatives of sirolimus 未知

    公开(公告)号：NZ568304A

    公开(公告)日：2011-07-29

    申请号：NZ56830406

    申请日：2006-12-12

    Applicant: ABBOTT LAB

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

    IPC: C07D498/18 ,  A61K31/395

    Abstract: Disclosed is a method of preparing a rapamycin derivative zotarolimus molecule of formula I comprising: (a) reacting a molecule of formula II: with triflic anhydride to produce a molecule of the triflate and (b) reacting the molecule of the triflate with a molecule of formula IV: wherein R1 is selected from the group consisting of =O, and (H, OH); R2 and R5 are independently selected from the group consisting of H, -C(=O)R6, -C(=O)OR6, -C(=O) NHR6 and -C(=S)OR6; R3 is selected from the group consisting of =O and OR5; or R2 and R3 can be taken together to form moiety of formula A -C(R7)(R8) -O-B, where A is a bond to oxygen bonded to carbon 28 and B is a bond bonded to carbon 26 as defined above; R4 is selected from the group consisting of H and alkyl; R6 is selected from the group consisting of alkyl, cycloalkyl, aryl groups, and heterocyclic groups; R7 and R8 are independently selected from the group consisting of H, alkyl, or R7 and R8 taken together are =O R9 and R10 are independently selected from the group consisting of H, alkenyl, alkenylcycloalkenyl, alkenylcycloalkyl, alkyl, alkylcycloalkenyl, alkylcycloalkyl, alkynyl, aralkyl, aryl, cycloalkenyl, cycloalkyl, cycloalkylalkyl, cycloalkylcycloalkyl, cycloalkenylalkyl, heterocyclyl, and combinations thereof, wherein the reactions are performed in a single pot.

    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    35.
    发明专利
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 未知

    公开(公告)号：CA2936497A1

    公开(公告)日：2007-08-23

    申请号：CA2936497

    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 ,  A61K31/436

    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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