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1. (WO2018085962) BASE ACETAMIDE GLYCERIN ETHER MOLECULE, CHEMICAL SYNTHESIS METHOD THEREFOR, AND APPLICATIONS THEREOF IN FIELD OF GENE THERAPY

Pub. No.:    WO/2018/085962    International Application No.:    PCT/CN2016/000712
Publication Date: Fri May 18 01:59:59 CEST 2018 International Filing Date: Wed Dec 28 00:59:59 CET 2016
IPC: C07D 473/34
C07D 473/18
C07D 239/54
C07D 239/47
A61K 9/127
A61K 48/00
C12N 15/88
Applicants: PEKING UNIVERSITY
北京大学
Inventors: YANG, Zhenjun
杨振军
WANG, Chao
王超
SUN, jing
孙晶
Title: BASE ACETAMIDE GLYCERIN ETHER MOLECULE, CHEMICAL SYNTHESIS METHOD THEREFOR, AND APPLICATIONS THEREOF IN FIELD OF GENE THERAPY
Abstract:
Disclosed in the present invention are a base acetamide glycerin ether molecule, a chemical synthesis method therefor, and applications thereof in the field of gene delivery. The molecule has an amphiphilic structure represented by formula (I), that is, a base-1-acetic acid is used as a hydrophilic head, and an amide bond is connected to glycerol aliphatic ether serving as a hydrophobic tail, so as to form an amphiphilic molecule. The Base group is common nature purine and a pyrimidine base, and the R group is a saturated or unsaturated aliphatic carbon chain. The compound can be prepared by means of an activated derivative of the base-1-acetic acid and 2, 3-dialkoxyl-1-propylamine, prices of the raw materials are low, and the synthesis method is simple. The compound can be used to prepare liposome and other supramolecular structures, and does not have obvious cytotoxicity. The base of the head of the compound can be combined with nucleic acid, and can carry the nucleic acid to enter a cell membrane. Accordingly, the compound has the potential of becoming a new non-cationic gene vector, and can be widely used in the field of gene therapy.