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    • 22. 发明授权
    • Process for the preparation of
4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2)
    • 制备4-氨基-1-苯基-c-乙氧基羰基 - 环己烯的方法(2)
    • US4008233A
    • 1977-02-15
    • US528107
    • 1974-11-29
    • Gerhard SatzingerManfred Herrmann
    • Gerhard SatzingerManfred Herrmann
    • C07D211/14C07D211/34C07D295/155C07C101/38C07D295/14
    • C07D295/155C07D211/14C07D211/34
    • This invention relates to 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen or alkyl having 1 to 4 carbon atoms, or one of the two groups is allyl, phenalkyl having 7 to 9 carbon atoms or .alpha.-methyl-.beta.-hydroxyethyl; or R.sub.1 and R.sub.2 together form a morpholino group, piperazino group substituted at the 4- position by methyl, benzyl, phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-phenethyl or benzoyl, or a piperidino group substituted at the 4- position by hydroxyl, phenyl, 2-methoxyphenyl, 4-methoxyphenyl, methyl or benzyl and medically acceptable addition compounds derived from inorganic and organic acids or lower alkyl halides. The compounds of the present invention are prepared by separation of 4-amino-1-phenyl-1-ethoxycarbonyl-cyclohexenes-(2), described in U.S. Patent Application Ser. No. 226,509, filed Feb. 15, 1972, into the two possible geometrical isomers. The instant compounds, the 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I, exhibit marked analgesic and neuroleptic activities and are useful for the alleviation and reduction of pain.
    • 本发明涉及式I的4r-氨基-1t-苯基-c-乙氧基羰基 - 环己烯 - (2):其中R 1和R 2相同或不同,为氢或具有1至4个碳原子的烷基, 或两个基团中的一个为烯丙基,具有7至9个碳原子的苯基烷基或α-甲基-β-羟乙基; 或R 1和R 2一起形成吗啉代基,在4-位上被甲基,苄基,苯基,3-氯苯基,4-氯苯基,2-苯乙基或苯甲酰基取代的哌嗪基或在4-位取代的哌啶子基, 羟基,苯基,2-甲氧基苯基,4-甲氧基苯基,甲基或苄基,以及衍生自无机和有机酸或低级烷基卤的医药上可接受的加成化合物。 本发明的化合物是通过分离美国专利申请序列号中描述的4-氨基-1-苯基-1-乙氧基羰基 - 环己烯 - (2)制备的。 1972年2月15日提交的226,509号的两种可能的几何异构体。 本发明化合物,式I的4r-氨基-1t-苯基1c-乙氧基羰基 - 环己烯 - (2)表现出明显的镇痛和精神安定活性,并且可用于缓解和减轻疼痛。