公开(公告)号：US20230416280A1

公开(公告)日：2023-12-28

申请号：US18252305

申请日：2021-11-08

申请人： STELLA PHARMA CORPORATION

发明人： Yusuke MURATA ,  Yoichiro OHTA ,  Hiroshi TAKENAKA ,  Kensuke SUZUKI

IPC分类号： C07F5/02

CPC分类号： C07F5/025

摘要： A method for producing 4-borono-L-phenylalanine and its intermediates is provided. The method is for producing a substituted phenyl compound represented by formula (II) from a substituted phenyl compound represented by formula (I). The method comprises a first step in which the compound represented by formula (I) reacts with a linear or branched C1-C10 alkylmagnesium halide in the presence of a metal halide; and a second step in which a boronic acid ester or boronic acid amide reacts with the compound obtained in said first step. The method also can comprise a step of deprotecting the compound of formula (II) obtained in the second step.

公开(公告)号：US20240239816A1

公开(公告)日：2024-07-18

申请号：US18563110

申请日：2022-04-20

申请人： STELLA PHARMA CORPORATION

发明人： Yusuke MURATA ,  Hiroshi TAKENAKA ,  Yoichiro OHTA ,  Aya SUDANI ,  Miki ISHIMURA ,  Kensuke SUZUKI ,  Hiroyuki KAI

IPC分类号： C07F5/02 ,  A61K41/00 ,  A61K51/04

CPC分类号： C07F5/025 ,  A61K41/0095 ,  A61K51/0402

摘要： Provided are new compounds that can have the property of being specifically taken up into cancer cells. In the present invention, novel 4-borono-phenylalanine derivatives, borono-phenylalanine derivatives having a heterocyclic skeleton, borono-phenylalanine derivatives having a fused ring structure, or pharmaceutically acceptable salts thereof are prepared. These compounds have the property of being taken up specifically by LAT1 and thus easily taken up specifically by cancer cells in the evaluation of LAT1 and LAT2 selective uptake, and can be conveniently used for neutron capture therapy and the like. A typical example is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.