Therapeutically useful tetralin derivatives
    4.
    发明授权
    Therapeutically useful tetralin derivatives 失效
    治疗上有用的四氢化萘衍生物

    公开(公告)号:US5214156A

    公开(公告)日:1993-05-25

    申请号:US866391

    申请日:1992-04-10

    摘要: This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## wherein YR.sub.1 is OR.sub.1 at the 8 position where R.sub.1 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3-8 cycloalkyl);R.sub.4 is hydrogen, C.sub.1-8 alkyl, --CH.sub.2 --(C.sub.3-4 cycloalkyl), --(CH.sub.2).sub.m --R.sub.5 or --CH.sub.2 --CH.sub.2 --X--(CH.sub.2).sub.n CH.sub.3 ; n is zero to 3 and m is 2 or 3; X is oxygen or sulfur;R.sub.5 is phenyl, C.sub.1-3 alkoxy, C.sub.1-3 alkyl, 2-thiophene, 3-thiophene, or phenyl substituted with one or two substituent groups selected from chlorine, bromine or fluorine; and with the proviso that when R.sub.3 contains more than four carbon atoms and R.sub.4 is alkyl, said alkyl contains from 1 to 3 carbon atoms.Alternatively, --YR.sub.1 is --S--(C.sub.1-3 alkyl) at the 5, 6, 7 or 8 position of the aromatic ring or OR.sub.1 at the 8 position where R.sub.1 is selected from the group consisting of C.sub.1-8 alkyl, C.sub.2-8 alkenyl, --CH.sub.2 --(C.sub.3-8 cycloalkyl) or benzyl;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3) alkyl;R.sub.3 is --CH.sub.2 --(C.sub.3 -C.sub.8) cycloalkyl;R.sub.4 is --(CH.sub.2).sub.m --(2-thiophenyl or 3-thiophenyl); and m is 2 or 3.

    摘要翻译: 本发明是治疗上有用的式Ⅰ化合物及其药学上可接受的酸加成盐,其中YR1为OR1,其中R1为-CH2-(C3-8环烷基); R2是氢或C1-3烷基; R3是-CH2-(C3-8环烷基); R 4是氢,C 1-8烷基,-CH 2 - (C 3-4环烷基), - (CH 2)m -R 5或-CH 2 -CH 2 -X-(CH 2)n CH 3; n为0〜3,m为2或3; X是氧或硫; R5是苯基,C1-3烷氧基,C1-3烷基,2-噻吩,3-噻吩或被一个或两个选自氯,溴或氟的取代基取代的苯基; 并且条件是当R 3含有多于4个碳原子且R 4是烷基时,所述烷基含有1至3个碳原子。 或者,-YR1是芳环的5,6,7或8位的-S-(C1-3烷基)或在8位的OR1,其中R1选自C1-8烷基,C2- 8链烯基,-CH 2 - (C 3-8环烷基)或苄基; R2是氢或(C1-C3)烷基; R3是-CH2-(C3-C8)环烷基; R4是 - (CH2)m-(2-噻吩基或3-噻吩基); m为2或3。

    Process for preparation of 4-mercapto-1-naphthol compounds
    6.
    发明授权
    Process for preparation of 4-mercapto-1-naphthol compounds 失效
    4-巯基-1-萘酚化合物的制备方法

    公开(公告)号:US5693846A

    公开(公告)日:1997-12-02

    申请号:US693838

    申请日:1996-08-01

    摘要: A process for preparation of 4-mercapto-1-naphthol compounds which comprises the steps of: (i) obtaining a 4-heterocyclylthio-1-naphthol compound by reacting a 1-naphthol compound with a heterocyclylsulfur chloride or by reacting a 4-iodo-1-naphthol compound with an alkali metal or ammonium salt of a mercaptoheterocyclic compound, (ii) hydrolyzing the resulting 4-heterocyclylthio-1-naphthol compound in the presence of a base to form a reaction product, and (iii) acidifying said reaction product. The resulting compounds are useful as intermediates in the synthesis of bleach accelerator releasing couplers for use in silver halide color photographic materials.

    摘要翻译: 一种制备4-巯基-1-萘酚化合物的方法,其包括以下步骤:(i)通过使1-萘酚化合物与杂环硫酰氯反应获得4-杂环硫基-1-萘酚化合物,或通过使4-碘代 -1-萘酚化合物与巯基杂环化合物的碱金属盐或铵盐反应,(ii)在碱的存在下水解所得4-杂环硫基-1-萘酚化合物以形成反应产物,和(iii)酸化所述反应 产品。 所得化合物可用作合成用于卤化银彩色照相材料的漂白促进剂释放成色剂的中间体。