Process for the production of 2,6-diaminobenzonitrile derivatives
    4.
    发明授权
    Process for the production of 2,6-diaminobenzonitrile derivatives 失效
    2,6-二氨基苄腈衍生物的制备方法

    公开(公告)号:US4504660A

    公开(公告)日:1985-03-12

    申请号:US395520

    申请日:1982-07-06

    CPC分类号: C07C255/00

    摘要: 2,6-Diaminobenzonitriles, useful in the production of N-(2-cyano-3-substituted or unsubstituted amino-phenyl)oxamate and N-(2-cyano-3-substituted or unsubstituted amino-phenyl)tetrazole-5-carboxamide antiallergy and antisecretory agents, are prepared by sequential displacement of the fluoro substituents from 2,6-difluorobenzonitrile with the appropriately substituted amine.

    摘要翻译: 可用于制备N-(2-氰基-3-取代或未取代的氨基 - 苯基)草酸酯和N-(2-氰基-3-取代或未取代的氨基 - 苯基)四唑-5-甲酰胺的2,6-二氨基苯腈 抗过敏和抗分泌剂,通过用适当取代的胺将2,6-二氟苄腈中的氟取代基顺序置换而制备。

    N-Benzyl and N-substituted benzyl tetrazole-5-carboxylic acids and the
preparation thereof
    6.
    发明授权
    N-Benzyl and N-substituted benzyl tetrazole-5-carboxylic acids and the preparation thereof 失效
    N-苄基和N-取代的苄基四唑-5-羧酸及其制备

    公开(公告)号:US4316037A

    公开(公告)日:1982-02-16

    申请号:US761149

    申请日:1977-01-21

    IPC分类号: C07D257/04 C07D257/02

    CPC分类号: C07D257/04

    摘要: N-Protected-tetrazole-5-carboxylic acid derivatives of the formula: ##STR1## in which R is --OM, halo or lower alkoxy wherein M is hydrogen, an alkali metal or an alkaline earth metal; andR.sub.1 is phenyl, 4-methoxyphenyl, 2,4-dimethoxyphenyl or 2,4,6-trimethoxyphenyl,are produced by addition of R.sub.1 --CH.sub.2 --N.sub.3 to a lower alkyl cyanoformate followed by saponification, optional acidification, and conversion to the carbonyl halide. The N-protected tetrazole-5-carbonylhalides are intermediates for the production of anti-allergic agents.

    摘要翻译: 其中R为-OM,卤素或低级烷氧基,其中M为氢,碱金属或碱土金属的N-保护的四唑-5-羧酸衍生物。 R1为苯基,4-甲氧基苯基,2,4-二甲氧基苯基或2,4,6-三甲氧基苯基,是通过将R1-CH2-N3加成到氰基甲酸低级烷基酯中进行皂化,任选酸化,并转化成羰基 卤化物。 N-保护的四唑-5-羰基卤化物是用于生产抗过敏剂的中间体。

    2-Cyano-3-or 4-(substituted amino)oxanilic acid derivatives
    7.
    发明授权
    2-Cyano-3-or 4-(substituted amino)oxanilic acid derivatives 失效
    2-氰基-3-或4-(取代的氨基)恶烷酸衍生物

    公开(公告)号:US4054591A

    公开(公告)日:1977-10-18

    申请号:US710481

    申请日:1976-08-04

    CPC分类号: C07D295/155 C07D265/26

    摘要: The 2-cyano-3-or 4-(substituted amino)oxanilic acid derivatives of the formula: ##STR1## in which the group ##STR2## appears in the designated 3- or 4- position and R is -H; an alkali metal; .sup.+ NH.sub.4 ; alkyl of 1 to 6 carbon atoms, inclusive; aralkyl of 7 or 8 carbon atoms; or cycloalkyl of 5 or 6 carbon atoms;R.sup.1 is --H or alkyl of 1 to 9 carbon atoms;R.sup.2 is --H, alkyl of 1 to 9 carbon atoms or cycloalkyl of 3 to 6 carbon atoms;R.sup.1 and R.sup.2, together, with the nitrogen atom to which they are attached, are aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-lower alkyl-piperazinyl, morpholino or thiomorpholino; and pharmaceutically acceptable acid addition salts thereof are anti-allergic agents.

    摘要翻译: 下式的2-氰基-3-或4-(取代氨基)草氨酸衍生物:其中基团出现在指定的3-或4-位,R为-H; 碱金属; + NH4; 含1-6个碳原子的烷基; 7或8个碳原子的芳烷基; 或5或6个碳原子的环烷基; R1是-H或1至9个碳原子的烷基; R2为-H,1〜9个碳原子的烷基或3〜6个碳原子的环烷基; R 1和R 2与它们所连接的氮原子一起是氮丙啶基,氮杂环丁烷基,吡咯烷基,哌啶基,哌嗪基,4-低级烷基 - 哌嗪基,吗啉代或硫代吗啉代; 及其药学上可接受的酸加成盐是抗过敏剂。