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    Preparation of 3-aryl and 3-aralkyl 6-sulfamyl-7-halo-1,3,4-tetrahydro-4-quinazolinone
    7.
    发明授权
    Preparation of 3-aryl and 3-aralkyl 6-sulfamyl-7-halo-1,3,4-tetrahydro-4-quinazolinone 失效
    3-芳基和3-芳烷基6-氨磺酰基-7-卤代-1,3,4-四氢-4-喹唑啉酮的制备

    公开(公告)号：US3862949A

    公开(公告)日：1975-01-28

    申请号：US31570272

    申请日：1972-12-15

    申请人： PENNWALT CORP

    发明人： SHETTY BOLA VITHAL

    IPC分类号： C07D239/95 ,  C07D51/48

    CPC分类号： C07D239/95

    摘要： A process for preparing 3-aryl and 3-aralkyl-6-sulfamyl-1,2,3,4tetrahydro-4-quinazolinone compounds suitable for use as diuretics, and particularly a process for preparing 2-methyl-3-otolyl-6-sulfamyl-7-chloro-1,2,3,4-tetrahydro-4-quinazolinone, by reacting a 5-halo-2-lower alkyl aniline with a lower alkyl haloformate to produce a N-carbalkoxy-5-halo-2-lower alkyl aniline, reacting said compound with a halosulfonic acid and ammonium hydroxide to produce N-carbalkoxy-5-halo-2-lower alkyl4-sulfamyl aniline, reacting said sulfamyl aniline with potassium permanganate to produce N-carbalkoxy-4-halo-5-sulfamyl anthranilic acid, reacting said anthranilic acid compound with a cyclizing and condensing agent such as thionyl chloride to produce 7-chloro-6-sulfamyl-isatoic anhydride, reacting said isatoic anhydride with toluidine or other like aryl or aralkyl amine to produce the corresponding benzamide, and reacting said benzamide with a suitable cyclizing agent su;ch as an acetal, aldehyde or ketone to produce the desired diuretic quinazolinone compound.

    摘要翻译： 适用于利尿剂的3-芳基和3-芳烷基-6-氨磺酰-1,2,3,4-四氢-4-喹唑啉酮化合物的制备方法，特别是制备2-甲基-3-邻 - 甲苯基-6-氨磺酰基-7-氯-1,2,3,4-四氢-4-喹唑啉酮，通过5-卤代-2-低级烷基苯胺与卤代甲酸低级烷基酯的反应生成N-烷烃氧基-5 - 卤代-2-低级烷基苯胺，使所述化合物与卤代磺酸和氢氧化铵反应，生成N-烷基烷氧基-5-卤代-2-低级烷基-4-氨磺酰苯胺，使所述的氨磺酰苯胺与高锰酸钾反应生成N- 烷基氧基-4-卤代-5-磺酰氨基邻氨基苯甲酸，使所述邻氨基苯甲酸化合物与环化缩合剂如亚硫酰氯反应，生成7-氯-6-氨磺酰基 - 丙酸酐，使所述的丙烯酸酐与甲苯胺或其它类似芳基 或芳烷基胺以产生相应的苯甲酰胺，并使所述苯甲酰胺与合适的环化剂su; ch作为缩醛，醛 r酮以产生所需的利尿喹唑啉酮化合物。

    Halo-sulfamylspiro- and dialkyl-quinazolinones
    10.
    发明授权
    Halo-sulfamylspiro- and dialkyl-quinazolinones 失效
    HALO-SULFAMYLSPIRO-和DIALKYL-QUINAZOLINONES

    公开(公告)号：US3637698A

    公开(公告)日：1972-01-25

    申请号：US3637698D

    申请日：1968-03-11

    申请人： PENNWALT CORP

    发明人： SHETTY BOLA VITHAL

    IPC分类号： C07D471/10 ,  C07D51/48

    CPC分类号： C07D471/10 ,  Y10S514/869

    摘要： A 7''HALO-6''-SULFAMYLSPIRO- OR DIALKYL-4,2''(1''H)-QUINAZOLIN-4''(3''H)-ONE, HAVING THE SPIRO GROUP IN THE 2-POSITION, HYDROGEN OR ALKYL IN THE 3-POSITION, AND HYDROGEN, ALKYL, AMINO, HALOGEN OR HALOLOWERALKYL IN THE 5- AND 8-POSITIONS. THE HYDROGENS OF THE SULFAMYL GROUP MAY BE SUBSTITUED BY ALKYL OR PHENYLALKYL OR TOGERTHER FORM A CARBOCYCLIC OR HETEROCYCLIC RING. THE SPIRO GROUP CAN BE COMPOSED ENTIRELY OF CARBON ATOMS OR CAN CONTAIN ONE OR MORE HETERO ATOMS, ESPECIALLY SULFUR, NITROGEN OR OXYGEN. THE COMPOUNDS ARE USEFUL IN DIURETICS AND SALURETICS.