Aryloxy-alkyl-dialkylamines
    2.
    发明授权
    Aryloxy-alkyl-dialkylamines 失效
    芳氧基 - 烷基 - 二烷基胺

    公开(公告)号:US6005102A

    公开(公告)日:1999-12-21

    申请号:US161653

    申请日:1998-09-28

    CPC分类号: C07D295/088 C07C217/48

    摘要: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.n --.

    摘要翻译: 本发明提供了可用于合成生物活性化合物的化合物及其制备方法,具有下式的化合物:其中:R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A是O或S; m为1〜3的整数,优选为2; R 3,R 4,R 5和R 6独立地选自H,卤素,-NO 2,烷基,烷氧基,C 1 -C 6全氟烷基,OH或其C 1 -C 4酯或其烷基醚,-CN,-O-R 1, O-Ar,-S-R 1,-S-Ar,-SO-R 1,-SO-Ar,-SO 2 -R 1,-SO 2 -Ar,-CO-R 1,-CO-Ar,-CO 2 -R -CO 2 -Ar; 并且Y选自a)部分:其中R 7和R 8独立地选自H,C 1 -C 6烷基或苯基; 或b)任选取代的五元,六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环,其含有至多两个选自-O - , - NH - , - N(C 1 -C 4烷基) - , - N =和-S(O)n - 。

    Aryloxy-alkyl-dialkylamines
    6.
    发明授权
    Aryloxy-alkyl-dialkylamines 失效
    芳氧基 - 烷基 - 二烷基胺

    公开(公告)号:US06268504B1

    公开(公告)日:2001-07-31

    申请号:US09458317

    申请日:1999-12-10

    IPC分类号: C07D27704

    CPC分类号: C07D295/088 C07C217/48

    摘要: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.

    摘要翻译: 本发明提供了可用于合成生物活性化合物的化合物及其制备方法,具有下式的化合物:其中:R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A是O或S; m为1〜3的整数,优选为2; R 3,R 4,R 5和R 6独立地选自H,卤素,-NO 2,烷基,烷氧基,C 1 -C 6全氟烷基,OH或其C 1 -C 4酯或其烷基醚,-CN,-O-R 1, O-Ar,-S-R 1,-S-Ar,-SO-R 1,-SO-Ar,-SO 2 -R 1,-SO 2 -Ar,-CO-R 1,-CO-Ar,-CO 2 -R -CO 2 -Ar; 并且Y选自a)部分:其中R 7和R 8独立地选自H,C 1 -C 6烷基或苯基; 或b)任选取代的五元,六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环,其含有至多两个选自-O - , - NH - , - N(C 1 -C 4烷基) - , - N =和-S(O)n - 。

    Preparation and purification of 4-(indazol-3-yl)phenols
    8.
    发明授权
    Preparation and purification of 4-(indazol-3-yl)phenols 失效
    制备和纯化4-(吲唑-3-基)苯酚

    公开(公告)号:US07601847B2

    公开(公告)日:2009-10-13

    申请号:US11257344

    申请日:2005-10-24

    IPC分类号: C07D231/56

    CPC分类号: C07D231/56

    摘要: The present invention concerns processes for the production and purification of compounds of the formula: where R1-R10 are as defined in the specification. Preferred processes of the invention utilize a lithium bis(trimethylsilyl)amide, lithium dicyclohexylamide, or potassium bis(trimethylsilyl)amide base and a R1—X alkylating agent where X is as described in the specification. An alcohol preferably is added to the product solution is used to promote crystallization of the desired product.

    摘要翻译: 本发明涉及生产和纯化下式化合物的方法:其中R1-R10如说明书中所定义。 本发明的优选方法使用双(三甲基甲硅烷基)氨基锂,二环己基氨基锂或二(三甲基甲硅烷基)氨基钾酰胺碱和R1为-X-烷基化剂,其中X如说明书中所述。 将优选加入到产物溶液中的醇用于促进所需产物的结晶。