Process for preparing a diastereomer of an optically active ester or amide of (cis-1,2-epoxypropyl)-phosphonic acid
    2.
    发明授权
    Process for preparing a diastereomer of an optically active ester or amide of (cis-1,2-epoxypropyl)-phosphonic acid 失效
    制备光学活性酯或(CIS-1,2-环氧丙基) - 磷酸的酰胺的二异氰酸酯的方法

    公开(公告)号:US3595869A

    公开(公告)日:1971-07-27

    申请号:US3595869D

    申请日:1968-05-15

    申请人: MERCK & CO INC

    发明人: SHUMAN RICHARD F

    IPC分类号: C07F9/655 C07D1/20

    CPC分类号: C07F9/65505

    摘要: A PROCESS FOR PREPARING A DIASTEREOMER OF AN OPTICALLYACTIVE ESTER OR AMIDE OF (CIS-1,2-EPOXYPROPYL) PHOSPHONIC ACID, WHICH COMPRISES SEPARATING ENANTIOMERS OR DIASTEREOMERS OF AN ESTER, AN AMIDE OR A SALT OF SAID ESTER OF AMIDE DERIVATIVE OF (CIS-1,2-EPOXYPROPYL)PHOSPHONIC ACID ENANTIOMERS. THE DERIVATIVES OF THE OPTICALLY-ACTIVE ISOMERS OF (CIS-1,2-EPOXYPROPYL) PHOSPHONIC ACID CAN THEN BE CONVERTED TO (CIS-1,2-EPOXYPROPYL)PHOSPHONIC ACID ENANTIOMERS OR A SALT THEREOF. (-) (CIS-1,2-EPOXYPROPYL) PHOSPHONIC ACID AND ITS SALTS ARE ACTIVE ANTIBIOTICS, WHICH ARE EFFECTIVE AGAINST VARIOUS GRAM-NEGATIVE AND GRAMPOSITIVE PATHOGENS.

    Process for separating enantiomers of (cis-1,2-epoxypropyl)phosphonic acid
    3.
    发明授权
    Process for separating enantiomers of (cis-1,2-epoxypropyl)phosphonic acid 失效
    (CIS-1,2-环氧丙基)磷酸的分离方法

    公开(公告)号:US3595881A

    公开(公告)日:1971-07-27

    申请号:US3595881D

    申请日:1968-05-15

    申请人: MERCK & CO INC

    发明人: SHUMAN RICHARD F

    IPC分类号: C07F9/655 C07D1/20

    CPC分类号: C07F9/65505

    摘要: MIXTURES OF (+) AND (-) (CIS-1,2-EPOXYPROPYL)-PHOSPHONIC ACID OR A SALT THEREOF ARE REACTED WITH A METAL SALT OF AN OPTICALLY-ACTIVE ACID OR WITH A METAL SALT OF A MIXTURE OF OPTICALLY-ACTIVE ACID ENANTIOMERS TO PRODUCE A METAL SALT OF (CIS-1,2-EPOXYPROPYL)SHPSHPONIC ACID CONTAINING A GREATER PROPORTION OF ONE OF THE ENANTIOMERS OF (CIS-1,2-EPOXYPROPYL)PHOSPHONIC ACID. THE PROCESS IS USEFUL FOR PREPARING MIXTURES OF THE ENANTIOMERIC FORMS OF (CIS-1,2-EPOXYPROPYL)PHOSPHONIC ACID CONTAINING A GREATER PROPORTION OF THE (-) ENANTIOMER, WHICH IS AN ANTIBIOTIC SUBSTANCE ACTIVE AGAINST VARIOUS GRAM-POSITIVE AND GRAMNEGATIVE PATHOGENS.

    2-sulfonyloxyethyl 3-trifluoromethylphenoxy-4{40 -chlorophenyl acetate
    4.
    发明授权
    2-sulfonyloxyethyl 3-trifluoromethylphenoxy-4{40 -chlorophenyl acetate 失效
    2-三氟乙酰基3-三氟甲基苯氧基-4 {40-氯代乙酰基乙酸酯

    公开(公告)号:US3923855A

    公开(公告)日:1975-12-02

    申请号:US41006273

    申请日:1973-10-26

    申请人: MERCK & CO INC

    发明人: SHUMAN RICHARD F

    摘要: A method for the preparation of 2-acetamidoethyl (3trifluoromethylphenoxy)(4-chlorophenyl)acetate which comprises treating a 2-substituted ethyl (3-trifluoromethylphenoxy)(4chlorophenyl)acetate with an N-substituted salt of acetamide. The 2-acetamidoethyl (3-trifluoromethylphenoxy)(4chlorophenyl)acetate obtained is a hypocholesterolemic and hypolipemic agent which effectively reduces the concentration of cholesterol, triglycerides and other lipids in blood serum.

    摘要翻译: 一种制备2-乙酰氨基乙基(3-三氟甲基苯氧基)(4-氯苯基)乙酸酯的方法,其包括用N-取代的乙酰胺盐处理2-取代的(3-三氟甲基苯氧基)(4-氯苯基)乙酸乙酯。 获得的2-乙酰氨基乙基(3-三氟甲基苯氧基)(4-氯苯基)乙酸酯是一种降低胆固醇,甘油三酯和其他血脂浓度的低胆固醇血症和降血脂药。

    Cyanomethyl(3-trifluoromethylphenoxy)(4-chlorophenyl)acetate
    6.
    发明授权
    Cyanomethyl(3-trifluoromethylphenoxy)(4-chlorophenyl)acetate 失效
    氰基(3-三氟甲基苯氧基)(4-氯苯乙烯)乙酸酯

    公开(公告)号:US3860628A

    公开(公告)日:1975-01-14

    申请号:US27144772

    申请日:1972-07-13

    申请人: MERCK & CO INC

    发明人: SHUMAN RICHARD F

    CPC分类号: C07C59/68 C07C68/02 C07C69/96

    摘要: A method for the preparation of 2-acetamidoethyl(3trifluoromethylphenoxy)(4-chlorophenyl)acetate which comprises treating 2-aminoethyl (3-trifluoromethylphenoxy)-(4chlorophenyl)acetate with an acetylating agent. The 2acetamidoethyl(3-trifluoromethylphenoxy)(4-chlorophenyl)-acetate thus obtained is a hypocholesterolemic and hypolipemic agent which effectively reduces the concentration of cholesterol, triglycerides and other lipids in blood serum.

    摘要翻译: 一种制备2-乙酰氨基乙基(3-三氟甲基苯氧基)(4-氯苯基)乙酸酯的方法,其包括用乙酰化剂处理2-氨基乙基(3-三氟甲基苯氧基) - (4-氯苯基)乙酸酯。 由此获得的2-乙酰氨基乙基(3-三氟甲基苯氧基)(4-氯苯基) - 乙酸酯是有效降低血清中胆固醇,甘油三酯和其他脂质的浓度的低胆固醇血症和降血脂药。