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1. (WO2018180917) METHOD FOR PRODUCING POLYOXYETHYLENE DERIVATIVE HAVING HYDROXY GROUPS AT TERMINAL

Pub. No.:    WO/2018/180917    International Application No.:    PCT/JP2018/011497
Publication Date: Fri Oct 05 01:59:59 CEST 2018 International Filing Date: Fri Mar 23 00:59:59 CET 2018
IPC: C08G 65/32
A61K 47/60
C08G 65/28
Applicants: NOF CORPORATION
日油株式会社
Inventors: YOSHIOKA Hiroki
吉岡 宏樹
YAMAMOTO Yuji
山本 裕二
Title: METHOD FOR PRODUCING POLYOXYETHYLENE DERIVATIVE HAVING HYDROXY GROUPS AT TERMINAL
Abstract:
Provided is a method for industrially producing a polyoxyethylene derivative (1) having a plurality of hydroxy groups at a terminal. The method, which is for producing a polyoxyethylene derivative represented by formula (1), comprises steps (A), (B), (C), and (D): step (A) in which a polyhydric alcohol having five or seven hydroxy groups is subjected to a hydroxy-protecting reaction to protect four or six of the hydroxy groups by forming a cyclic benzylidene acetal, thereby obtaining a compound that has a hydroxy group at the 1-position and has a protective group having a cyclic benzylidene acetal structure; step (B) in which ethylene oxide is polymerized with the compound obtained in step (A), in an amount of 11 to 3,650 mol to obtain a polyoxyethylene derivative; step (C) in which the terminal hydroxy group of the polyoxyethylene derivative obtained in step (B) is converted to a functional group reactive with a physiologically active substance; and step (D) in which the protective group of the polyoxyethylene derivative is removed. (In formula (1), L1 is a divalent linker; X is a functional group reactive with a physiologically active substance; a is 1 or 2; and n is 11-3,650.)