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26 条记录 (耗时 0.013 秒)

    Method for the preparation of (cis-1,2-epoxypropyl)-phosphonic acid and derivatives
    4.
    发明授权
    Method for the preparation of (cis-1,2-epoxypropyl)-phosphonic acid and derivatives 失效
    （CIS-1,2-环氧丙基） - 磷酸和衍生物的制备方法

    公开(公告)号：US3584014A

    公开(公告)日：1971-06-08

    申请号：US3584014D

    申请日：1969-06-02

    申请人： MERCK & CO INC

    发明人： FIRESTONE RAYMOND A ,  SLETZINGER MEYER

    IPC分类号： C07F9/38 ,  C07F9/655

    CPC分类号： C07F9/65505 ,  C07F9/3808

    摘要： A METHOD FOR THE PREPARATION OF (CIS-1,2-EPOXYPROPYL)PHOSPHONIC ACID AND ITS SALT AND ESTER DERIVATIVES, WHICH COMPRISES TREATING A ((1 - VINYLOXY) METHYL) PHOSPHONIC ACID OR A SALT OR ESTER THEREOF WITH A REAGENT CAPABLE OF EFFECTING RING CLOSURE. THE (CIS-1,2-EPOXYPROPYL) PHOSPHONIC ACID PRODUCT THUS OBTAINED AND ITS SALTS ARE ANTIBIOTICS WHICH HAVE UTILITY ASS ANTIMICROBIAL AGENTSS IN INHIBITING THE GROWTH OF GRAM-POSITIVE AND GRAM-NEGATIVE PATHOGENIC BATERIA.

    Method of preparing (cis-1,2-epoxypropyl)phosphonic acid esters
    6.
    发明授权
    Method of preparing (cis-1,2-epoxypropyl)phosphonic acid esters 失效
    制备（CIS-1,2-环氧丙基）磷酸酯酯的方法

    公开(公告)号：US3679711A

    公开(公告)日：1972-07-25

    申请号：US3679711D

    申请日：1969-01-27

    申请人： MERCK & CO INC

    发明人： FIRESTONE RAYMOND A

    IPC分类号： C07F9/655 ,  C07F9/40

    CPC分类号： C07F9/65505

    摘要： A method for the preparation of (cis-1,2-epoxypropyl)-phosphonic acid and its salts and ester derivatives which comprises treating a propionaldehyde substituted in the 2-position by a leaving group with: (1) an alkali metal dihydrocarbylphosphite, (2) a trihydrocarbylphosphite or (3) a di-alkali metal phosphite. Suitable leaving groups include halogen, alkarylsufonyloxy, alkanesulfonyloxy or a sulfonium, sulfoxonium, ammonium or phosphonium cation. The (cis-1,2-epoxypropyl)phosphonic acid product thus obtained and its salts are antibiotics which have utility as antibacterials in inhibiting the growth of gramnegative and gram-positive pathogenic bacteria.

    摘要翻译： （顺式-1,2-环氧丙基）膦酸及其盐和酯衍生物的制备方法，其包括用离去基团处理在2-位取代的丙醛：（1）碱金属二烃基亚磷酸酯（ 2）亚磷酸三烃基酯或（3）二碱金属亚磷酸酯。 合适的离去基团包括卤素，烷芳基磺酰氧基，烷磺酰氧基或锍，氧化锍，铵或鏻阳离子。 由此获得的（顺式-1,2-环氧丙基）膦酸产物及其盐是抗生素，其可用作抑制革兰氏阴性和革兰氏阳性致病细菌生长的抗菌剂。

    A method for the preparation of (cis-1,2-epoxypropyl) phosphonic acid products
    7.
    发明授权
    A method for the preparation of (cis-1,2-epoxypropyl) phosphonic acid products 失效
    （CIS-1,2-环氧丙基）磷酸产品的制备方法

    公开(公告)号：US3678078A

    公开(公告)日：1972-07-18

    申请号：US3678078D

    申请日：1969-01-29

    申请人： MERCK & CO INC

    发明人： FIRESTONE RAYMOND A

    IPC分类号： C07F9/141 ,  C07F9/146 ,  C07F9/46 ,  C07F9/48 ,  C07F9/655 ,  C07F9/40 ,  C07F9/42

    CPC分类号： C07F9/65505 ,  C07F9/1411 ,  C07F9/146 ,  C07F9/46 ,  C07F9/48

    摘要： A method for the preparation of (cis-1,2-epoxypropyl)-phosphonic dihalide and esters of (cis-1,2-epoxypropyl)-phosphonic acid, which comprises treating 2-hydroxypropionaldehyde with phosphorous trihalide or an ester of phosphorohalidous acid to afford, respectively, (1-formylethyl)-phosphorodihalidite or (1formylethyl)phosphite, followed by the rearrangement of the said intermediates to yield (cis-1,2-epoxypropyl)phosphonic dihalide or (cis-1,2-epoxypropyl)phosphonate. The dihalide and esterified products thus obtained have utility as intermediates inasmuch as they may be converted by conventional means to (cis-1,2epoxypropyl)phosphonic acid or to the salts thereof, which products are antibiotics useful in inhibiting the growth of gramnegative and gram-positive pathogenic bacteria.

    摘要翻译： 制备（顺式-1,2-环氧丙基） - 膦酸二卤化物的方法和（顺式-1,2-环氧丙基） - 膦酸的酯，其包括用三卤化磷或卤代磷酸酯处理2-羟基丙醛至 分别加入（1-甲基乙基） - 磷酸二卤化物或（1-甲基乙基）亚磷酸酯，然后重新排列所述中间体，得到（顺式-1,2-环氧丙基）膦酸二卤化物或（顺式-1,2-环氧丙基） 膦酸盐。 由此获得的二卤化物和酯化产物可用作中间体，因为它们可以通过常规方法转化为（顺式-1,2-环氧丙基）膦酸或其盐，该产物是可用于抑制革兰氏阴性菌生长的抗生素， 阴性和革兰氏阳性病原菌。