Title:
METHOD FOR PREPARING SUBSTITUTED PHENYLACETIC ACID DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2019/047654
Kind Code:
A1
Abstract:
The present invention belongs to the field of drug synthesis, and relates to a method for preparing a substituted phenylacetic acid derivative, specifically a method for preparing 2-[4-(2-oxopentylmethyl)phenylpropionic acid]. A precursor compound (I) of loxoprofen is prepared by reacting a dihalobenzyl compound or a disubstituted benzyl compound with a cyclopentanone group or a precursor compound thereof, wherein X is a halogen, L1 is a halogen, OH, OMs, OTs or OTf, L2 is a halogen, a cyano, a hydroxyl, -CH2OH, -CHO, nitromethane, an ester group, -NR4R5, OTf, OTs, OMs, -C=CR6 or -C≡CR7, R4, R5, R6 and R7 are a low substituted alkyl, Z is a cyclopentanone group or a precursor form thereof, the precursor form being (II), (III), (IV), (V) or (VI), and R3 is a low substituted alkyl. Further, the method comprises a step of converting the precursor form of the cyclopentanone group to the cyclopentanone group. The precursor compound of loxoprofen is used for preparing loxoprofen compounds.
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Inventors:
LI JIEPING (CN)
GAO ZHAOBO (CN)
CHAI BING (CN)
ZHENG HUI (CN)
LIU SHENGMIN (CN)
LIU AQING (CN)
GUO BIBAO (CN)
ZHENG JUNCHENG (CN)
WANG CHANGFA (CN)
LU WEIWEI (CN)
GAO ZHAOBO (CN)
CHAI BING (CN)
ZHENG HUI (CN)
LIU SHENGMIN (CN)
LIU AQING (CN)
GUO BIBAO (CN)
ZHENG JUNCHENG (CN)
WANG CHANGFA (CN)
LU WEIWEI (CN)
Application Number:
PCT/CN2018/099121
Publication Date:
March 14, 2019
Filing Date:
August 07, 2018
Export Citation:
Assignee:
JIANGSU RUIKE MEDICAL SCIENCE AND TECH CO LTD (CN)
International Classes:
C07C59/86; C07C51/08
Foreign References:
| CN101412670A | 2009-04-22 | |||
| CN104326903A | 2015-02-04 | |||
| JP2000327603A | 2000-11-28 | |||
| US4161538A | 1979-07-17 | |||
| CN105017009A | 2015-11-04 | |||
| CN104710309A | 2015-06-17 | |||
| CN201710800788A | 2017-09-07 | |||
| US4161538A | 1979-07-17 | |||
| US5681979A | 1997-10-28 |
Other References:
DATABASE Registry 30 November 2006 (2006-11-30), Database accession no. 914358-39-7
See also references of EP 3680227A4
See also references of EP 3680227A4
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