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    Process for making and isolating (R)-2-hydroxy-4-phenylbutyric acid and esters
    28.
    发明授权
    Process for making and isolating (R)-2-hydroxy-4-phenylbutyric acid and esters 失效
    制备和分离（R）-2-羟基-4-苯基丁酸和酯的方法

    公开(公告)号：US4837354A

    公开(公告)日：1989-06-06

    申请号：US96312

    申请日：1987-09-09

    申请人： Gary A. Flynn ,  Douglas W. Beight

    发明人： Gary A. Flynn ,  Douglas W. Beight

    IPC分类号： C07C59/48

    CPC分类号： C07C59/48

    摘要： Disclosed herein is a novel compound, (L)-menthyl 2-oxo-4-phenylbutyrate, and an improved process for making and isolating a substantially pure compound of the structural formula: ##STR1## wherein Y is hydrogen or (L)-menthyl the improvement which comprises: (a) stereoselectively reducing (L)-menthyl 2-oxo-4-phenylbutyrate by contacting said compound with S-B-(3-pinanyl)-9 horabicyclo[3,3,1]nonone,(b) stereoselectively isolating (L)-menthyl-(R)-2-hydroxy-4-phenylbutyrate by crystallization, and optionally hydrolyzing the so obtained ester;and further comprises optionally esterifying the so obtained acid by contacting said acid with a C.sub.1 -C.sub.6 alkanol in presence of acid.

    摘要翻译： 本文公开了一种新型化合物（2-甲基-2-氧代-4-苯基丁酸酯），以及制备和分离基本上纯的结构式化合物的改进方法：其中Y为氢或（L） - 薄荷基 其改进包括：（a）通过使所述化合物与SB-（3-蒎烷基）-9二氢[3,3,1]壬酮，（b）立体选择性地接触，立体选择性地还原（L） - 2-氧代-4-苯基丁酸乙酯 通过结晶分离（L） - 薄荷基 - （R）-2-羟基-4-苯基丁酸酯，并任选地水解所得酯; 并且还包括任选地通过在酸存在下使所述酸与C 1 -C 6烷醇接触来酯化所得酸。

    Sparsomycin derivatives
    29.
    发明授权
    Sparsomycin derivatives 失效
    孢子霉素衍生物

    公开(公告)号：US4595687A

    公开(公告)日：1986-06-17

    申请号：US632133

    申请日：1984-07-18

    申请人： Douglas W. Beight ,  Gary A. Flynn

    发明人： Douglas W. Beight ,  Gary A. Flynn

    IPC分类号： C07D263/10 ,  A61K31/496 ,  A61K31/505 ,  A61P31/04 ,  A61P33/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/54 ,  C07D263/14 ,  C07D307/64 ,  C07D401/12 ,  C07D405/12 ,  C07D239/10

    CPC分类号： C07D239/54

    摘要： Sparsomycin derivatives of the formula ##STR1## wherein X and Y are each independently an oxo or an imino group; n is 0 or the integer 1 or 2; R.sub.1 is a hydrogen or 1 to 4 carbon alkyl group; R.sub.2 is a hydrogen, a 1 to 4 carbon alkyl, a 2 to 5 carbon acyl or a benzoyl group; and R is a 1 to 6 carbon alkyl, 3 to 8 carbon alkenyl, cyanomethyl carboxymethyl, carbalkoxymethyl wherein the alkoxy moiety is a 1 to 4 carbon alkoxy group, nitromethyl, alkylcarbonylmethyl wherein the alkyl moiety is a 1 to 4 carbon alkyl group, pyridyl, furanyl, or furfuryl group or a phenyl or benzyl group optionally substituted by a methylenedioxy or one to two halogen, 1 to 4 carbon alkyl, 1 to 4 carbon alkoxy, 1 to 4 carbon alkylthio, hydroxy, nitro or cyano groups or a pharmaceutically acceptable acid addition salt thereof. Also described are their use as antiprotozoals and antibacterials.

    摘要翻译： 其中X和Y各自独立地是氧代基或亚氨基的式“IMAGE”的孢子霉素衍生物; n为0或整数1或2; R 1是氢或1-4个碳的烷基; R2是氢，1至4个碳烷基，2至5个碳酰基或苯甲酰基; R为碳原子数1〜6的烷基，碳原子数为3〜8的烯基，氰基甲基羧甲基，烷氧基甲基，烷氧基部分为1〜4个碳原子的烷氧基，硝基甲基，烷基部分为1〜4个碳烷基的烷基羰基甲基，吡啶基 ，呋喃基或糠基或任选被亚甲二氧基或一至二个卤素，1-4个碳烷基，1至4个碳烷氧基，1至4个碳烷硫基，羟基，硝基或氰基取代的苯基或苄基。 其可接受的酸加成盐。 还描述了它们作为抗原生动物和抗菌剂的用途。