发明名称 TYROSINE DERIVATIVE AND METHOD FOR PRODUCING TYROSINE DERIVATIVE
摘要 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.
申请公布号 US2014187814(A1) 申请公布日期 2014.07.03
申请号 US201314141721 申请日期 2013.12.27
申请人 NARD Institute, Ltd. 发明人 NAKAO Hidekazu;HOSHINO Junichi;OGATA Tokutaro;MIYASHITA Naoki;YAMAMOTO Yoshikazu
分类号 C07C229/36;C07C227/16 主分类号 C07C229/36
代理机构 代理人
主权项 1. A tyrosine derivative represented by the following formula (I):wherein R1 is a hydrogen atom or a protective group for the amino group; R2 is a hydrogen atom or a protective group for the carboxy group; R3 is a hydrogen atom or a C1-6 alkyl group; R4 is a halogen atom, a hydroxy group, a C1-6 alkyl group, a C1-6 halogenated alkyl group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, an aryl group optionally having substituent α, a heterocyclic group optionally having substituent α, a C1-6 alkoxy group, a C1-6 alkylthio group, a C1-6 halogenated alkoxy group or a C7-13 aralkyloxy group optionally having substituent α; A is —(CH2)l—[Z(CH2)m]n— wherein Z is an amino group, an ether group, a thioether group, a carbonyl group, a thionyl group, an ester group, an amide group, a urea group or a thiourea group; l is an integer of not less than 1 and not more than 6; m is an integer of not less than 1 and not more than 4; and n is an integer of not less than 0 and not more than 4; X is a leaving group selected from the group consisting of a chlorine atom, a bromine atom, an iodine atom, a methanesulfonyloxy group, a trifluoromethanesulfonyloxy group, a chloromethanesulfonyloxy group, an ethanesulfonyloxy group, a benzenesulfonyloxy group and a toluenesulfonyloxy group; substituent α is one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, a cyano group, a thiol group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 halogenated alkyl group and a C1-6 alkylthio group; provided that the position of R4 is para to the position of the X-A-O— group.
地址 Amagasaki-shi JP