Precursors and synthesis of methyl-9-oxo-11.alpha.,
16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoates
    103.
    发明授权
    Precursors and synthesis of methyl-9-oxo-11.alpha., 16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoates 失效
    甲基-9-氧代-11α,16-二羟基-16-乙烯基-5-顺式-13-反 - 前列腺素的前体和合成

    公开(公告)号:US4958037A

    公开(公告)日:1990-09-18

    申请号:US185621

    申请日:1988-04-25

    摘要: Novel precursors for the synthesis of methyl-9-oxo-11.alpha.,16-dihydroxy-16-vinyl-5-cis-13-trans prostadienoates having the formulae ##STR1## wherein R.sub.1 is H or C.sub.1 -C.sub.4 alkyl; R.sub.2 is C.sub.1 -C.sub.4 alkyl, R.sub.3 is H, C.sub.1 -C.sub.4 trialkylsilyl or C.sub.1 -C.sub.6 alkyl; X.sub.1 is halogen, cyano, C.sub.1 -C.sub.4 alkoxycarbonyl, carboxy or tri (C.sub.1 -C.sub.4 alkoxy)methyl; n is 2-4 inclusive; and P.sub.1 is H or a blocking or protective group; congeners and racemic mixture of these compounds and processes of synthesizing them.

    摘要翻译: 用于合成具有下式的甲基-9-氧代-11α,16-二羟基-16-乙烯基-5-顺式-13-反式前列腺素的新型前体(IMAGE)(2)(3)( (4b)其中R1是H或C1-C4烷基; R2是C1-C4烷基,R3是H,C1-C4三烷基甲硅烷基或C1-C6烷基; X 1为卤素,氰基,C 1 -C 4烷氧基羰基,羧基或三(C 1 -C 4烷氧基)甲基; n为2-4; P1为H或封端或保护基团; 这些化合物的同源物和外消旋混合物以及它们的合成方法。

    3-phenyl-2-propeneamine derivatives, their preparation and composition
containing them
    110.
    发明授权
    3-phenyl-2-propeneamine derivatives, their preparation and composition containing them 失效
    3-苯基-2-丙烯胺衍生物,它们的制备方法和含有它们的组合物

    公开(公告)号:US4755599A

    公开(公告)日:1988-07-05

    申请号:US10558

    申请日:1987-02-03

    摘要: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.7 =H or alkylcarbonyl, alkyloxycarbonyl, alkylaminocarbonyl or benzoyl, optionally substituted by one or two halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 groups,(ii) or Y and A together form a 1-hydroxycycloalkyl radical, the ring of which contains 5 or 6 C, optionally joined to a benzene ring,it being understood that the alkyl radicals and alkyl parts contains 1 to 4 C as a straight or branched chain, and that the invention relates to all the possible geometric and optical isomers as well as their mixtures.These compounds are useful as antidepressants.

    摘要翻译: 本发明提供下式的化合物:其中R = H,卤素,烷基,烷氧基,链烯基,NH 2,烷基氨基,二烷基氨基或CF 3,R 3 = H或烷基,R 4和R 5 = H,R 1和 R 2 = H或烷基,任选被烯基(2至4 C)取代,或者R 1和R 2一起形成含有4至7个环成员的饱和杂环,并任选地含有另外的杂原子,例如任选被烷基取代的O,S或N, 或R4 = H,R1 = H或烷基,R2和R5一起形成亚烷基(3至4 C)基团,和(i)A =烷基或苯基,其未被取代或被一个或两个选自卤素,烷基 ,烷氧基,烷硫基,NH 2,烷基氨基,二烷基氨基,NO 2或CF 3,或者A =吡啶基,苄基或环烷基(3至6 C),Y = S,SO或SO 2或基团:其中R 6 = H或烷基,且R7 = H或烷基羰基,烷氧基羰基,烷基氨基羰基或苯甲酰基,任选被一个或两个卤素,烷基,烷氧基,烷硫基,NH 2, 烷基氨基,二烷基氨基,NO 2或CF 3基团,(ii)或Y和A一起形成1-羟基环烷基,其环包含5或6个C,任选地连接到苯环,应理解烷基和烷基 部分包含1至4 C作为直链或支链,本发明涉及所有可能的几何和光学异构体及其混合物。 这些化合物可用作抗抑郁药。