2-vinyl-1 4-dihydroquinazoline derivatives
    83.
    发明授权
    2-vinyl-1 4-dihydroquinazoline derivatives 失效
    2-乙烯基-1,4-二氢吲哚啉衍生物

    公开(公告)号:US3631035A

    公开(公告)日:1971-12-28

    申请号:US3631035D

    申请日:1969-04-02

    申请人: PFIZER

    发明人: COX DAVID A

    IPC分类号: C07D239/74 C07D51/48

    CPC分类号: C07D239/74 Y10S514/822

    摘要: A SERIES OF NOVEL 1,4-DISUBSTITUTED-2-VINYL-1,4-DIHYDROQUINAZOLINE DERIVATIVES, INCLUDING THEIR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS, HAVE BEEN PREPARED USING VARIOUS ALTERNATE SYNTHETIC ROUTES. THESE COMPOUNDS ARE USEFUL IN THE EFFECTIVE CONTROL AND/OR PREVENTION OF THROMBOSIS. TRANS-1,4-DIMETHYL-2-STYRYL-1,4-DIHYDROQUINAZOLINE AND TRANS - 1 - METHYL-2-STYRYL-4-PHENYL-1,4-DIHYDROQUINAZOLINE ARE PREFERRED EMBODIMENTS.

    Novel synthesis of 2-quinazolinepropionic acids and derivatives
    84.
    发明授权
    Novel synthesis of 2-quinazolinepropionic acids and derivatives 失效
    2-喹唑啉衍生物和衍生物的新合成

    公开(公告)号:US3595861A

    公开(公告)日:1971-07-27

    申请号:US3595861D

    申请日:1967-12-08

    IPC分类号: C07D487/04 C07D51/48

    CPC分类号: C07D487/04

    摘要: THIS INVENTION IS CONCERNED WITH 2-QUINAZOLINEPROPIONIC ACIDS, AND DERIVATIVES THEREOF, WHICH ARE PHARMACOLOGICALLY EFFICACIOUS AS TRANQUILIZING AGENTS. FURTHER, IT RELATES TO 5HYDROXYTETRAHYDROPYRROLOQUINAZOLINONES WHICH ARE USEFUL INTERMEDIATES IN THE PREPARATION OF THESE 2-QUINAZOLINEPORPIONIC ACIDS. STILL FURTHER, IT RELATES TO A PROCESS FOR THE PREPARATION OF THESE 2-QUINAZOLINEPROPIONIC ACIDS AND ESTERS. THE REACTION IS EFFECTED BY CONTACTING AN APPROPRIATE 2''-CARBONYL-3-HALOPROPIONANILIDE (I) WITH AN ALKALI METAL CYANIDE (II), E.G., SODIUM AND POTASSIUM CYANIDE, AND A REACTANT (III) SELECTED FROM THE GROUP CONSISTING OF WATER, AN ALKANOL AND A GLYCOL AT A TEMPERATURE RANGE FROM ABOUT 50*C. TO ABOUT REFLUX TEMPERATURES FOR A PERIOD OF ABOUT TEN TO ABOUT TWENTY-FOUR HOURS.