公开(公告)号：US20140187814A1

公开(公告)日：2014-07-03

申请号：US14141721

申请日：2013-12-27

Applicant: NARD Institute, Ltd.

Inventor： Hidekazu NAKAO ,  Junichi HOSHINO ,  Tokutaro OGATA ,  Naoki MIYASHITA ,  Yoshikazu YAMAMOTO

IPC: C07C229/36 ,  C07C227/16

CPC classification number: C07C229/36 ,  C07C227/16 ,  C07C271/22 ,  Y02P20/55

Abstract: The objective of the present invention is to provide a tyrosine derivative which is useful as a melatonin MT1 receptor antagonist, and a method for producing a specific tyrosine derivative with high yield by efficiently introducing an iodine atom at the para position of the phenolic hydroxy group in the benzene ring of tyrosine with good regioselectivity. The tyrosine derivative of the present invention is characterized in being represented by the following formula (I): wherein R1 is a protective group of the amino group and the like; R2 is a protective group of the carboxy group and the like; R3 is a hydrogen atom and the like; R4 is a halogen atom and the like; A is —(CH2)l—[Z(CH2)m]n—; X is a leaving group.

Abstract translation: 本发明的目的是提供可用作褪黑激素MT1受体拮抗剂的酪氨酸衍生物，以及通过在酚羟基的对位有效引入碘原子而以高产率制备特异性酪氨酸衍生物的方法 酪氨酸苯环具有良好的区域选择性。 本发明的酪氨酸衍生物的特征在于由下式（I）表示：其中R1是氨基的保护基等; R2是羧基等的保护基; R3是氢原子等; R4是卤素原子等; A是 - （CH 2）1 - [Z（CH 2）m] n - X是离职小组。