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    • 2. 发明公开
    • PROCESS FOR THE PREPARATION OF OXAZOLIDINONE DERIVATIVE
    • VERFAHREN ZUR HERSTELLUNG VON OXAZOLIDINON-DERIVATEN
    • EP1118611A1
    • 2001-07-25
    • EP99944807.9
    • 1999-09-24
    • NIPPON CHEMIPHAR CO., LTD.
    • YAMAMOTO, MasaoYOSHIDA, Shinichi
    • C07D263/22
    • C07D263/20C07D263/22
    • The invention relates to a process for preparing (5RS)-5-benzyl-3-[(1SR)-3-morpholino-1-phenylpropyl]-1,3-oxazolidin-2-one or its pharmacologically acceptable salt which is of value as a remedy for treatment of incontinence of urine and thamuria and which is performed by the steps of:

      dissolving an acid and a mixture of (2RS)-1- [(1SR)-3-morpholino-1-phenylpropyl]amino-3-phenyl-2-propanol and (2RS) -1- ((lRS,) -3-morpholino-1-phenylpropyl] amino-3-phenyl-2-propanol in a solvent to obtain a salt of the former (1SR)-compound utilizing difference of solubility between the salt of (1SR)-compound and a salt of the latter (1RS)-compound;
      bringing a basic compound into contact with the salt of (1SR)-compound to produce a free (1SR)-compound;
      reacting thus produced (2RS)-1-[(1SR)-3-morpholino-1-phenylpropyl]amino-3-phenyl-2-propanol with a compound having the formula (I):

              R 2 C=O     (I)

      wherein R represents a chlorine atom, an alkoxy group, an aryloxy group or an amino group, or a chloroformic acid ester; and
      cyclizing the resulting product.
    • 本发明涉及制备(5RS)-5-苄基-3-Ä(1SR)-3-吗啉代-1-苯基丙基] -1,3-恶唑烷-2-酮或其药理学上可接受的盐的方法,其值为 用于治疗尿和性尿失禁的治疗方法,其通过以下步骤进行:将酸和(2RS)-1-Ä(1SR)-3-吗啉代-1-苯基丙基氨基-3-苯基-2 丙醇和(2RS)-1 - ((1R,3R)-3-吗啉代-1-苯基丙基)氨基-3-苯基-2-丙醇在溶剂中反应,得到前者(1SR) - 化合物的盐,利用溶解度差异 (1SR) - 化合物的盐和后者的盐(1RS) - 化合物之间;使碱性化合物与(1SR)化合物的盐接触以产生游离(1SR) - 化合物;如此制备的(1SR) 2RS)-1-Ä(1SR)-3-吗啉代-1-苯基丙基氨基-3-苯基-2-丙醇与具有式(I)的化合物反应:R2C = O其中R表示氯原子,烷氧基, 芳氧基或氨基,或氯仿a 碳酸酯 并使所得产品环化