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45 条记录 (耗时 0.018 秒)

    Synthesis of lithium aminoborohydrides and reactions thereof
    2.
    发明授权
    Synthesis of lithium aminoborohydrides and reactions thereof 失效
    氨基硼氢化锂的合成及其反应

    公开(公告)号：US5466798A

    公开(公告)日：1995-11-14

    申请号：US138612

    申请日：1993-10-15

    申请人： Bakthan Singaram ,  Gary B. Fisher ,  Joseph C. Fuller ,  John Harrison ,  Christian T. Goralski

    发明人： Bakthan Singaram ,  Gary B. Fisher ,  Joseph C. Fuller ,  John Harrison ,  Christian T. Goralski

    IPC分类号： C07C213/00 ,  C07C215/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D223/02 ,  C07D207/00 ,  C07F5/02

    CPC分类号： C07D295/096 ,  C07C213/00 ,  C07C215/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/092

    摘要： The present invention relates to novel, powerful reducing agents, lithium aminoborohydrides which are prepared by addition of BH.sub.3 .cndot.THF to the corresponding dialkylamine at 25.degree. C. to give the intermediate amineborane complex. Subsequent deprotonation by strong base, e.g. n-BuLi, yields the aminoborohydride quantitatively. Lithium aminoborohydrides are powerful reducing agents, comparable in strength to lithium aluminum hydride. The activity is determined by the dialkylamine. Lithium pyrrolidinoborohydride has unique activity and selectivity in its reducing properties. Esters, lactones and anhydrides are reduced cleanly at 25.degree. C. to give the corresponding alcohols, while carboxylic acids are not reduced. Test reductions show that lithium pyrrolidinoborohydride is also capable of reducing a wide range of functional groups including amides, epoxides, oximes, nitriles and halides.

    摘要翻译： 本发明涉及通过在25℃下向相应的二烷基胺中加入BH3.THF而制得的新的强大的还原剂氨基硼酸锂，得到中间体胺硼烷络合物。 随后通过强碱去质子化，例如 n-BuLi，定量产生氨基硼氢化钠。 氨基硼氢化锂是强大的还原剂，其强度与氢化铝锂相当。 活性由二烷基胺决定。 吡咯烷基硼氢化锂在还原性能方面具有独特的活性和选择性。 酯，内酯和酸酐在25℃下干净地还原，得到相应的醇，而羧酸不被还原。 测试减少表明，吡咯烷基硼氢化锂还能够减少宽范围的官能团，包括酰胺，环氧化物，肟，腈和卤化物。

    Asymmetric synthesis of .beta.-amino alcohols from chiral or achiral enamines
    3.
    发明授权
    Asymmetric synthesis of .beta.-amino alcohols from chiral or achiral enamines 失效
    手性或非手性烯胺对β-氨基醇的不对称合成

    公开(公告)号：US5367073A

    公开(公告)日：1994-11-22

    申请号：US138613

    申请日：1993-10-15

    申请人： Bakthan Singaram ,  Gary B. Fisher ,  Christian T. Goralski ,  Lawrence W. Nicholson

    发明人： Bakthan Singaram ,  Gary B. Fisher ,  Christian T. Goralski ,  Lawrence W. Nicholson

    IPC分类号： C07C213/00 ,  C07C215/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D207/12 ,  C07D295/08 ,  C07C213/38

    CPC分类号： C07D295/096 ,  C07C213/00 ,  C07C215/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/092

    摘要： The present invention relates to a process for the synthesis of chiral enantiomerically pure .beta.-amino alcohols which are extraordinarily important as therapeutic agents for the treatment of a variety of human disorders and as chiral auxiliaries in organic synthesis. The hydroboration of enamines is a versatile and convenient method for the synthesis of both racemic and enantiomerically pure .beta.-amino alcohols in high yields. This methodology enables the synthesis of virtually any .beta.-amino alcohol. Hydroboration of these enamines with chiral organic borohydrides, e.g. either mono- or diisopinocampheylborane, followed by oxidation with aqueous or solid NaOH/30% H.sub.2 O.sub.2 or Me.sub.3 NO, gives the corresponding chiral .beta.-amino alcohol. Enantiomeric excesses ranged from 60% for reactions run at 25.degree. C. to greater than 99% for reactions run at -25.degree. C.

    摘要翻译： 本发明涉及合成手性对映异构纯的β-氨基醇的方法，其作为用于治疗多种人类疾病的治疗剂非常重要，并且作为有机合成中的手性助剂。 烯胺的硼氢化合物是以高产率合成外消旋和对映异构纯的β-氨基醇的通用和方便的方法。 该方法使得几乎可以合成任何β-氨基醇。 这些烯胺与手性有机硼氢化物的水解，例如 单或二蒎烷基硼烷，然后用水或固体NaOH / 30％H 2 O 2或Me 3 NO 3氧化，得到相应的手性β-氨基醇。 在25℃下进行的反应，对映异构体的过量范围为60％，对于在-25℃下进行的反应为大于99％

    Stereospecific synthesis of [E]-alkenes from enamines via hydroboration
    5.
    发明授权
    Stereospecific synthesis of [E]-alkenes from enamines via hydroboration 失效
    通过氢化从烯胺的[E] - 烯烃的立体特异性合成

    公开(公告)号：US4886924A

    公开(公告)日：1989-12-12

    申请号：US258743

    申请日：1988-10-17

    申请人： Christian T. Goralski ,  Bakthan Singaram ,  Herbert C. Brown

    发明人： Christian T. Goralski ,  Bakthan Singaram ,  Herbert C. Brown

    IPC分类号： C07D333/08

    CPC分类号： C07D333/08

    摘要： A process for the stereospecific synthesis of [E] alkenes from enamines comprising the steps of hydroborating the enamine; esterifying the organoborane so formed and oxidizing the boronic ester in the presence of hydrogen peroxide and in the absence of added base under conditions sufficient to form the [E] alkene in high yield.

    摘要翻译： 从烯胺立体特异性合成[E]烯烃的方法，包括加氢烯胺的步骤; 酯化如此形成的有机硼烷，并在过氧化氢存在下和在不加入碱的情况下将硼酸酯氧化成足以以高产率形成[E]烯烃的条件。

    1-(ARYLTHIO, ARYLSULFINYL AND ARYLSULFONYL)-1,1-DIHALOMETHANESULFONAMIDES
    9.
    发明授权
    1-(ARYLTHIO, ARYLSULFINYL AND ARYLSULFONYL)-1,1-DIHALOMETHANESULFONAMIDES 失效
    1-（ARYLTHIO，ARYLSULFINYL和ARYLSULFONYL）-1,1-二缩水甘油醚

    公开(公告)号：US3946007A

    公开(公告)日：1976-03-23

    申请号：US554953

    申请日：1975-03-03

    申请人： Christian T. Goralski ,  Thomas C. Klingler

    发明人： Christian T. Goralski ,  Thomas C. Klingler

    IPC分类号： C07D211/10 ,  C07D295/26 ,  C07D295/22

    CPC分类号： C07D295/26 ,  C07D211/10

    摘要： The compounds of the formula ##SPC1##In which R is lower alkyl, lower alkoxy or halo, x is an integer from 0 to 2, n is an integer from 0 to 3, Y is halo and R.sub.1 and R.sub.2 independently are hydrogen, lower alkyl, phenyl or substituted phenyl, or, together with the nitrogen atom, form a heterocyclic ring also containing up to one oxygen atom in the heterocycle. The compounds in which x is 0 are prepared by adding chlorine or bromine to a 1-arylthiomethanesulfonamide in the presence of pyridine to form the 1-arylthio-1, 1-dihalomethanesulfonamide. The compounds in which x is 1 or 2 is prepared by adding sodium hypochlorite or sodium hypobromite to a 1-(arylsulfinyl)methane-sulfonamide or a 1-(arylsulfonyl)methanesulfonamide to form the 1-(arylsulfinyl)-1,1-dihalomethanesulfonamide or 1-(arylsulfonyl)-1,1-dihalomethanesulfonamide, respectively. The compounds are useful as antimicrobial agents.

    摘要翻译： 式中R为低级烷基，低级烷氧基或卤素的化合物，x为0至2的整数，n为0至3的整数，Y为卤素，R 1和R 2各为氢，低级烷基，苯基 或取代的苯基，或者与氮原子一起形成在该杂环中也含有至多一个氧原子的杂环。 在吡啶存在下，通过在1-芳基硫代甲磺酰胺中加入氯或溴来制备x为0的化合物，形成1-芳硫基-1,1-二卤代甲磺酰胺。 通过向1-（芳基亚磺酰基）甲磺酰胺或1-（芳基磺酰基）甲磺酰胺中加入次氯酸钠或次溴酸钠，形成1-（芳基亚磺酰基）-1,1-二卤代甲磺酰胺制备x为1或2的化合物 或1-（芳基磺酰基）-1,1-二卤代甲磺酰胺。 这些化合物可用作抗微生物剂。