Method of preparing isomers of bis isoquinolinium compounds
    3.
    发明授权
    Method of preparing isomers of bis isoquinolinium compounds 失效
    双异喹啉化合物异构体的制备方法

    公开(公告)号:US4491665A

    公开(公告)日:1985-01-01

    申请号:US253299

    申请日:1981-04-13

    CPC分类号: C07D217/20

    摘要: This invention provides the neuromuscular blocking agents of formula (I): ##STR1## where B and C are each a group of formula (II) and are meta or para to one another: ##STR2## wherein D is CH.sub.2 CH.sub.2 or CH.dbd.CH (preferably trans); Y is alkyl of 1-4 carbon atoms (methyl, ethyl, propyl or butyl); E and F and H or OCH.sub.3 ; X.sup.- is an anion, preferably pharmaceutically acceptable; and the substituted benzyl and substituted propyl groups are in a trans relationship relative to each other in the nitrogen-containing ring.Methods for preparing the compounds, pharmaceutical formulations containing the compounds, and their use are also described.

    摘要翻译: 本发明提供式(I)的神经肌肉阻滞剂:其中B和C各自是式(II)的基团,并且彼此是间位或对位的:其中D是CH 2 CH 2或CH = CH(优选反式); Y是1-4个碳原子的烷基(甲基,乙基,丙基或丁基); E和F以及H或OCH 3; X-是阴离子,优选药学上可接受的; 并且取代的苄基和取代的丙基在含氮环中彼此相互相互关系。 还描述了制备化合物的方法,含有该化合物的药物制剂及其用途。

    Benzyl cyanoacetals
    5.
    发明授权
    Benzyl cyanoacetals 失效
    苄基氰缩醛

    公开(公告)号:US4144263A

    公开(公告)日:1979-03-13

    申请号:US804537

    申请日:1977-06-08

    摘要: Benzyl cyanoacetals of formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R.sup.4 is an alkoxycarbonyl group, or an aldehyde group;And R.sup.5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an .alpha.-substituted-.beta.-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzyl-pyrimidine by reaction with guanidine.

    摘要翻译: 苄基氰基缩醛,其结构式如下:其中R 1,R 2和R 3相同或不同,各自为卤素或氢原子,烷氧基,烷基或二烷基氨基; R4是烷氧基羰基或醛基; 且R 5为烷基; 各自具有1至4个碳原子的烷基或烷氧基,以及它们在制备抗菌2,4-二氨基-5-苄基嘧啶中的用途。 它们由原酸酯和α-取代的β-苄基丙腈之间的反应制备,然后通过与胍反应将所得的氰基缩醛转化为苄基 - 嘧啶。

    Synthesis of leucovorin
    10.
    发明授权
    Synthesis of leucovorin 失效
    甲酰四氢叶酸的合成

    公开(公告)号:US4500711A

    公开(公告)日:1985-02-19

    申请号:US218554

    申请日:1980-12-22

    IPC分类号: C07D475/04

    CPC分类号: C07D475/04

    摘要: In the synthesis of calcium leucovorin (calcium 5-formyl-5,6,7,8-tetrahydrofolate), the use of an amine base in the conversion of anhydroleucovorin (5,10-methenyl-5,6,7,8-tetrahydrofolic acid) to leucovorin unexpectedly results in a pure (USP) product directly from the reaction mixture.

    摘要翻译: 在钙亚叶酸钙(5-甲酰基-5,6,7,8-四氢叶酸钙)的合成中,使用胺碱在脱氢氢化蛋白(5,10-甲基-5,6,7,8-四氢叶酸 酸)到甲酰四氢叶酸,意外地从反应混合物直接导致纯(USP)产物。