Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin
    1.
    发明授权
    Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin 有权
    从10-羟基-4-(S)喜树碱制备拓扑替康的方法

    公开(公告)号:US06660861B1

    公开(公告)日:2003-12-09

    申请号:US10401119

    申请日:2003-03-27

    IPC分类号: C07D49114

    CPC分类号: C07D491/22

    摘要: The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3′4′:6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.

    摘要翻译: 本发明涉及二卤代甲烷作为制备拓扑替康{4-(S)-10(二甲基氨基) - 甲基-4-乙基-4,9-二羟基-H-吡喃并[3'4':6,7 ]吲哚并[1,2-b]喹啉-3,14(4H,12H)二酮}。 本发明公开了在固 - 液相转移催化作用下二氯甲烷的理论应用,当其用作10-羟基-4-(S)氨基烷基化的C-1单元的来源时,其可以作为溶剂和反应物, 喜树碱

    Trichosporon sp RRLY-15 (DSM 11829) and its use to prepare S(+)-6-methoxy-methyl-2-naphthalene acetic acid
    2.
    发明授权
    Trichosporon sp RRLY-15 (DSM 11829) and its use to prepare S(+)-6-methoxy-methyl-2-naphthalene acetic acid 失效
    Trichosporon sp RRLY-15(DSM 11829)及其用于制备S(+) - 6-甲氧基 - 甲基-2-萘乙酸

    公开(公告)号:US06242243B1

    公开(公告)日:2001-06-05

    申请号:US09050011

    申请日:1998-03-30

    IPC分类号: C12N118

    摘要: This invention discloses a process for the use of a novel organism belonging to the genus Trichosporon sp. as whole wet or dry cell culture or cell free extract or crude enzyme or pure isolated enzyme The strain of Trichosporon sp. used in the process is designated as RRLY-15 and has been deposited in Deutsche Sammlung von Mikroorganismen und Zellekulturen GmbH (DSMZ). The invention also discloses the preparation of S(+)-6-methoxy-2-naphthalene acetic acid (naproxen) of formula (2) through enantioselective hydrolysis of a racemic mixture of alkyl esters of (±)-6-methoxy-&agr;-methyl-2-naphthalene acetic acid of formula (1) where R represents —CH3,—C2H5,—C3H7,—C4H9 and the like and S(+)- Naproxen is a medicinally important non steroidal anti-inflammatory drug.

    摘要翻译: 本发明公开了一种使用属于Trichosporon sp。的新生物的方法。 作为整个湿或干细胞培养或无细胞提取物或粗酶或纯分离的酶Trichosporon sp。 在该过程中使用的产品被指定为RRLY-15,并已存放在德意志银行(Mikroorganismen und Zellekulturen GmbH)(DSMZ)。 本发明还公开了通过对映选择性水解(±)-6-甲氧基-α-甲氧基-2-甲基苯基的烷基酯的外消旋混合物制备式(2)的S(+) - 6-甲氧基-2-萘乙酸(萘普生) 式(1)的甲基-2-萘乙酸,其中R表示-CH 3,-C 2 H 5,-C 3 H 7,-C 4 H 9等,而S(+) - 萘普生是药物重要的非甾体抗炎药。