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    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS
    22.
    发明专利
    ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF SIROLIMUS 未知

    公开(公告)号：CA2936497C

    公开(公告)日：2018-04-17

    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 a heptane/acetone column. The product-containing fractions are concentrated. The product is dissolved in .tau.-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.

    23.
    发明专利
    未知

    公开(公告)号：BRPI0619844A2

    公开(公告)日：2011-10-18

    申请号：BRPI0619844

    申请日：2006-12-12

    Applicant: ABBOTT LAB

    Inventor： DHAON MADHUP ,  HSIAO CHU-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.

    27.
    发明专利
    未知

    公开(公告)号：AT361913T

    公开(公告)日：2007-06-15

    申请号：AT01966367

    申请日：2001-08-29

    Applicant: ABBOTT LAB

    Inventor： CHEMBURKAR SANJAY ,  PATEL KETAN ,  SPIWEK HARRY

    IPC: C07D239/10 ,  C07B53/00 ,  C07D403/06 ,  C07D521/00

    Abstract: The instant invention provides processes and intermediates employed in the synthesis of ((2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2S-(1-tetrahydropyrimid-2-onyl)-3-methyl-butanoyl)amino-1,6-diphenylhexane and analogs thereof.

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