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Title:
METHOD FOR PRODUCING POLYOXYETHYLENE DERIVATIVE HAVING HYDROXY GROUPS AT TERMINAL
Document Type and Number:
WIPO Patent Application WO/2018/180917
Kind Code:
A1
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.)

Inventors:
YOSHIOKA HIROKI (JP)
YAMAMOTO YUJI (JP)
Application Number:
PCT/JP2018/011497
Publication Date:
October 04, 2018
Filing Date:
March 22, 2018
Export Citation:
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Assignee:
NOF CORP (JP)
International Classes:
A61K47/60; C08G65/32; C08G65/28
Domestic Patent References:
WO2012133490A12012-10-04
WO2010114074A12010-10-07
Foreign References:
JP2011157466A2011-08-18
JPH02231488A1990-09-13
JPS48043748B1
JPS57200381A1982-12-08
JP2012214747A2012-11-08
JP2017069699A2017-04-06
Other References:
ARTHUR T. NESSRAYMOND M. HANNC. S. HUDSON, J. AM. CHEM., vol. 75, 1953, pages 132 - 134
Attorney, Agent or Firm:
SHIN-EI PATENT FIRM, P.C. (JP)
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