Novel prostacyclin derivatives and a process for the preparation thereof

    公开(公告)号:US4692464A

    公开(公告)日:1987-09-08

    申请号:US352411

    申请日:1982-02-26

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 -alkylammonium, (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--;W is hydroxymethylene, RO-methylene, CH.sub.3 or CH.sub.3, ##STR2## wherein OH or OR is in the .alpha.- or .beta.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;D and E together are a direct bond, orD is C.sub.1-10 alkylene, C.sub.1-10 alkenylene or C.sub.1-10 alkynylene or one of these groups substituted by fluorine, andE is oxygen, --C.tbd.C-- or a direct bond;R.sub.2 is (a) a C.sub.1-10 hydrocarbon aliphatic radical, (b) a C.sub.6-10 hydrocarbon aliphatic radical substituted by C.sub.6-10 aryl or by C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; (c) C.sub.4-10 cycloalkyl, (d) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (e) C.sub.6-10 aryl, (f) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; andR.sub.3 is OH or OR; and, when R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.

    Smoking compositions containing a dioxane diester flavorant-release
additive
    86.
    发明授权
    Smoking compositions containing a dioxane diester flavorant-release additive 失效
    含有二恶烷二酯调味剂释放添加剂的吸烟组合物

    公开(公告)号:US4538628A

    公开(公告)日:1985-09-03

    申请号:US659464

    申请日:1984-10-10

    IPC分类号: A24B15/40 C07D319/12

    CPC分类号: A24B15/403 C07D319/12

    摘要: This invention provides smoking compositions which contain a dioxane diester compound as a flavorant additive.In one of its embodiments, this invention provides tobacco compositions which contain a dioxane diester flavorant additive such as 2,5-bis(3-methylvaleryloxy)-1,4-dioxane: ##STR1## Under cigarette smoking conditions the above illustrated dioxane diester pyrolyzes into 3-methylvaleric acid and other products which enhance the flavor of the mainstream smoke and the aroma of sidestream smoke.

    摘要翻译: 本发明提供含有二恶烷二酯化合物作为调味剂添加剂的吸烟组合物。 在其一个实施方案中,本发明提供了含有二恶烷二酯调味剂添加剂如2,5-双(3-甲基戊酰氧基)-1,4-二恶烷的烟草组合物:在吸烟条件下,上述二恶烷二酯热解 成为3-甲基戊酸等产品,增强主流烟味和侧流烟雾的香气。

    5-Bromo-5,5-dicarboxyethylvalaraldehyde diethyl acetal
    89.
    发明授权
    5-Bromo-5,5-dicarboxyethylvalaraldehyde diethyl acetal 失效
    5-溴-5,5-二羧基乙基戊醛二乙基缩醛

    公开(公告)号:US4172208A

    公开(公告)日:1979-10-23

    申请号:US928747

    申请日:1978-07-27

    摘要: The compound of the formula: ##STR1## is useful as an intermediate to prepare a compound having the generic formula ##STR2## wherein X is selected from groups to provide tetrahydropyran type compounds, 1,4 dioxane type compounds or tetrahydrofuran type compounds, and R is selected from the group consisting of alkali metal, NH.sub.4.sup.+, NH(CH.sub.2 CH.sub.2 OH).sub.3.sup.+, and lower alkyl, branched or straight chain, with up to about C.sub.20 in the chain, useful as a detergent builder.

    摘要翻译: 下式的化合物可用作制备具有通式“IMAGE”的化合物的中间体,其中X选自提供四氢吡喃型化合物,1,4-二恶烷型化合物或四氢呋喃型化合物,R 选自碱金属,NH 4 +,NH(CH 2 CH 2 OH)3+和低级烷基,支链或直链,链中至多约C20,可用作洗涤剂助洗剂。

    Process for preparing 1,4-dioxan-2-ones

    公开(公告)号:US4166821A

    公开(公告)日:1979-09-04

    申请号:US920438

    申请日:1978-06-29

    申请人: Shigeto Suzuki

    发明人: Shigeto Suzuki

    IPC分类号: C07C51/00 C07D319/12

    CPC分类号: C07D319/12 C07C51/00

    摘要: 1,4-Dioxan-2-ones are prepared by contacting carbon monoxide with formaldehyde, a 1,2-glycol, and a catalytic amount of hydrogen fluoride. The products of this reaction are readily converted into diglycolic acids by heating with aqueous caustic in the presence of a nickel catalyst.