Method for the manufacture of the
cis-2-hydroxy-2-phenyl-r-1-cyclohexanecarboxylic acid
    1.
    发明授权
    Method for the manufacture of the cis-2-hydroxy-2-phenyl-r-1-cyclohexanecarboxylic acid 失效
    顺式-2-羟基-2-苯基-r-1-环己烷羧酸的制备方法

    公开(公告)号:US4125558A

    公开(公告)日:1978-11-14

    申请号:US739715

    申请日:1976-11-08

    申请人: Cosimo B. Torsi

    发明人: Cosimo B. Torsi

    CPC分类号: C07D319/08

    摘要: A known effective choleretic, cis-2-hydroxy-2-phenyl-r-1-cyclohexane carboxylic acid is obtained with a novel method wherein 1-phenylcyclohexene is reacted with formaldehyde in formic acid or mixture of formic acid with other solvents. The reaction mixture is hydrolyzed (alkaline hydrolysis) to provide a substituted cyclohexanol concurrently with a substituted dioxan. The substituted diol is separated from the substituted dioxan and finally oxidized to obtain the expected acid.

    摘要翻译: 得到一种已知的有效的胆固醇顺式-2-羟基-2-苯基-r-1-环己烷羧酸,其中1-苯基环己烯与甲醛或甲酸与其它溶剂的混合物与甲醛反应。 将反应混合物水解(碱性水解)以与取代的二恶烷同时提供取代的环己醇。 将取代的二醇与取代的二恶烷分离,最后氧化得到预期的酸。

    Prostaglandin intermediates and optically active isomers thereof
    2.
    发明授权
    Prostaglandin intermediates and optically active isomers thereof 失效
    前列腺素中间体及其旋光异构体

    公开(公告)号:US3980700A

    公开(公告)日:1976-09-14

    申请号:US561647

    申请日:1975-03-24

    申请人: Masateru Miyano

    发明人: Masateru Miyano

    IPC分类号: C07C405/00 C07C65/14

    CPC分类号: C07C405/0041 C07C405/00

    摘要: The condensation of dimethyl 3-oxoundecane-1,11-dioate with styrylglyoxal affords 14-phenyl-9,12-dioxo-11-hydroxytetradec-13-enoic acid, which is cyclized to afford 3-hydroxy-5-oxo-2-styrylcyclopent-1-eneheptanoic acid. Hydroxylation of the styryl double bond affords the corresponding 2-(.alpha.,.beta.-dihydroxyphenethyl) derivative. Resolution of the racemic 2-styryl-3-hydroxy compounds with either (-) or (+)-O-methylmandelyl chloride yields the optically active isomers which are separated chromatographically. The instant compounds are useful as anti-microbial, anti-fungal and hypotensive agents, as prostaglandin (PGE.sub.2) antagonists and also as intermediates to prostanoic acid derivatives and their optically active isomers which exhibit anti-microbial, pepsin-inhibitory, hypotensive and smooth muscle-contracting properties.

    摘要翻译: 3-氧代十一烷-1,11-二酸二甲酯与苯乙烯基乙二醛的缩合得到14-苯基-9,12-二氧代-11-羟基十四碳-13-烯酸,将其环化得到3-羟基-5-氧代-2- 苯乙烯基环戊-1-烯庚酸。 苯乙烯基双键的羟基化得到相应的2-(α,β-二羟基苯乙基)衍生物。 用( - )或(+) - O-甲基对苯二甲酰氯拆分外消旋的2-苯乙烯基-3-羟基化合物,得到色谱分离的旋光异构体。 本发明的化合物作为前列腺素(PGE2)拮抗剂和前列腺酸衍生物及其旋光异构体的中间体可用作抗微生物,抗真菌和降血压药,其表现出抗微生物,胃蛋白酶抑制,降血压和平滑肌 - 收合属性。

    Phenyl-benzoic acid derivatives
    6.
    发明授权
    Phenyl-benzoic acid derivatives 失效
    苯基苯甲酸衍生物

    公开(公告)号:US3950380A

    公开(公告)日:1976-04-13

    申请号:US499042

    申请日:1974-08-20

    摘要: The present invention relates to a series of new compounds, their salts and esters and to methods for the preparation of the compounds having the general formula: ##SPC1##In which R.sub.1 represents a straight or branched C.sub.1 -C.sub.6 alkyl, alkenyl or alkynyl radical, or a C.sub.1 -C.sub.3 alkyl radical substituted with phenyl, halophenyl, trifluoromethylphenyl, (lower alkoxy)phenyl, or with a 5-membered or 6-membered heterocyclic ring containing not more than two heteroatoms selected from the group consisting of oxygen, sulphur and nitrogen; Ar stands for a phenyl radical, optionally being substituted with halogen, lower alkyl, hydroxy, or lower alkoxy; Y stands for O, S, NH or a CH.sub.2 radical; and YR.sub.1 is placed in the 2- or 3-position.The compounds of the invention which are valuable in the human and veterinary practice, possess a pronounced diuretic and/or saluretic activity.

    摘要翻译: 本发明涉及一系列新化合物,其盐和酯,以及制备具有以下通式的化合物的方法:其中R1表示直链或支链C1-C6烷基,烯基或炔基或C1 被苯基,卤代苯基,三氟甲基苯基,(低级烷氧基)苯基或与含有不多于两个选自氧,硫和氮的杂原子的5元或6元杂环取代的-C 3烷基; Ar代表苯基,任选被卤素,低级烷基,羟基或低级烷氧基取代; Y代表O,S,NH或CH2基; 并将YR1置于2-或3-位。

    Substituted phenylsulfonylmethyl salicylic acids and esters and salts thereof
    7.
    发明授权
    Substituted phenylsulfonylmethyl salicylic acids and esters and salts thereof 失效
    取代的苯磺酰甲基脂肪酸及其酯及其盐

    公开(公告)号:US3706792A

    公开(公告)日:1972-12-19

    申请号:US3706792D

    申请日:1970-04-20

    申请人: MERCK & CO INC

    CPC分类号: C07C317/00 Y10S514/916

    摘要: SUBSTITTED (BENZYLTHIO)-SALICYLIC ACIDS, (PHENYLMERCAPTOMETHYL)-SALICYLIC ACIDS AND PHENYL DISULFIDE SALICYLIC ACIDS AND THE NON-TOXIC PHARMACEUTICAL ACCEPTED SALTS, ESTERS, AMIDES AND VARIOUS DERIVATIVES THEREOF. ALSO A METHOD OF TREATING INFLAMMATION WHICH COMPRISES ADMINISTERING THE ABOVE COMPOUNDS AND VARIOUS DERIVATIVES ARE ALSO CLAIMED. THE SUBSTITURED (BENZYLTHIO) -SALICYLIC ACIDS, (PHENYLMERCAPTOMETHYL)-SALICYLIC ACIDS AND PHENYL DISULFIDE SALICYLIC ACIDS DESCRIBED HEREIN HVE ANTI-INFLAMMATORY, ANTI-PYRETIC AND ANALGESIC ACIVITY.