Method for synthesizing novel VHL ligand 4-F-VH032

Method for synthesizing novel VHL ligand 4-F-VH032

The invention belongs to the technical field of chemical synthesis, and relates to a method for synthesizing a novel VHL ligand 4-F-VH032 shown in a formula 1. The technical route for preparing the 4-F-VH032 is simple to operate, simple in route and high in yield, and all used reagents are common re...

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Hauptverfasser: WEI BANGGUO, MAO ZHUOYA, SI CHANGMEI, LIN GUOQIANG
Format: Patent
Sprache:chi ; eng
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator WEI BANGGUO
MAO ZHUOYA
SI CHANGMEI
LIN GUOQIANG
description The invention belongs to the technical field of chemical synthesis, and relates to a method for synthesizing a novel VHL ligand 4-F-VH032 shown in a formula 1. The technical route for preparing the 4-F-VH032 is simple to operate, simple in route and high in yield, and all used reagents are common reagents. According to the present invention, the VH032 is a VHL ligand, and is used for collecting the von Hippel-Lindau (VHL) protein; vH032 is a VHL/HIF-1alpha interaction inhibitor, and Kd is 185 nM. The VH032 can be connected with a target protein ligand through a linker to form a PROTAC molecule. 本发明属化学合成技术领域，涉及一种合成下式1的新型VHL配体4-F-VH032的方法。本发明所述制备4-F-VH032的技术路线，操作简单，路线简洁，收率较高，所用试剂均为常用试剂。本发明所述VH032是一种VHL配体，用于募集von Hippel-Lindau(VHL)蛋白。VH032是VHL/HIF-1α相互作用抑制剂，Kd为185nM。VH032可通过linker与靶蛋白配体连接，形成PROTAC分子。
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HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Method for synthesizing novel VHL ligand 4-F-VH032
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