申请人:Pascual Coca Gustavo
公开号:US20070254959A1
公开(公告)日:2007-11-01
The process comprises reacting a compound of formula (II), where R is a hydroxyl protecting group, and the asterisk indicates an asymmetric carbon atom, with diisopropylamine in the presence of a reducing agent; optionally converting the resulting intermediate into a salt and, if so desired, isolating it; removing the hydroxyl protecting group; and if so desired, separating the desired (R) or (S) enantiomer, or the mixture of enantiomers and/or converting the obtained compound into a pharmaceutically acceptable salt thereof. Tolterodine is a muscarinic receptor antagonist useful in treating urinary incontinence and other symptoms of urinary bladder hyperactivity.
该过程包括在还原剂存在下,将公式(II)化合物(其中R是羟基保护基,星号表示不对称碳原子)与二异丙基胺反应;可选择将所得中间体转化为盐,并如有需要,将其分离;去除羟基保护基;如果需要,分离所需的(R)或(S)对映体,或对映体的混合物和/或将所得化合物转化为其药用可接受的盐。托尔吡啶是一种肌动蛋白受体拮抗剂,可用于治疗尿失禁和其他尿膀胱过度活动的症状。