会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明授权
    • Process for preparing sertraline intermediates
    • 舍曲林中间体的制备方法
    • US4839104A
    • 1989-06-13
    • US207579
    • 1988-06-16
    • George J. QuallichMichael T. Williams
    • George J. QuallichMichael T. Williams
    • C07C45/46C07C45/59C07C49/697C07C51/09C07C51/367C07D307/33
    • C07D307/33C07C45/46C07C45/59C07C49/697C07C51/09C07C51/367
    • A novel three-step process for preparing 4-(3,4-dichlorophenyl)-4-phenylbutanoic acid is disclosed, which involves (1) reducing 4-(3,4-dichlorophenyl)-4-ketobutanoic acid to 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid; (2) then converting the intermediate hydroxy acid formed in the first step to 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone, and (3) thereafter reacting the resulting gamma-butyrolactone compound with benzene in a Friedel-Crafts type reaction to form the desired final product. The latter compound is known to be useful as an intermediate leading to 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone and ultimately, to cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalene amine (sertraline), which is known to be a preferred anti-depressant agent in the field of medicinal chemistry. The aforementioned 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone and 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid are both novel compounds. There is also disclosed a novel process for converting 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone directly to 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone, as well as an alternate novel process for converting 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid directly to this same key intermediate.
    • 公开了一种制备4-(3,4-二氯苯基)-4-苯基丁酸的新型三步法,其包括(1)将4-(3,4-二氯苯基)-4-酮丁酸还原成4-(3 ,4-二氯苯基)-4-羟基丁酸; (2)然后将第一步中形成的中间体羟基酸转化为5-(3,4-二氯苯基) - 二氢-2(3H) - 呋喃酮,和(3)然后使所得的γ-丁内酯化合物与苯在 Friedel-Crafts型反应形成所需的最终产品。 已知后一种化合物可用作导致4-(3,4-二氯苯基)-3,4-二氢-1(2H) - 萘酮的中间体,最终可用于顺式 - (1S)(4S)-N- 甲基-4-(3,4-二氯苯基)-1,2,3,4-四氢-1-萘色胺(舍曲林),已知它是药物化学领域中优选的抗抑郁剂。 上述5-(3,4-二氯苯基) - 二氢-2(3H) - 呋喃酮和4-(3,4-二氯苯基)-4-羟基丁酸都是新化合物。 还公开了一种将5-(3,4-二氯苯基) - 二氢-2(3H) - 呋喃酮直接转化为4-(3,4-二氯苯基)-3,4-二氢-1(2H) - 萘酮,以及将4-(3,4-二氯苯基)-4-羟基丁酸直接转化为该相同关键中间体的替代新方法。