Title:
METHOD FOR SYNTHESIZING ATORVASTATIN CALCIUM INTERMEDIATE BY USING MULTI-COMPONENT ONE-POT METHOD
Document Type and Number:
WIPO Patent Application WO/2022/048025
Kind Code:
A1
Abstract:
The present invention provides a method for synthesizing an atorvastatin calcium intermediate by using a multi-component one-pot method. Specifically, the present invention provides a one-pot synthesis method for 4-(4-fluorophenyl)-2-(2-methylpropanoyl)-3-phenyl-4-oxo-N-phenylbutanamide. The one-pot synthesis method is characterized in that a target compound is synthesized from N-phenyl phenylpropiolamide and 4-fluorobenzaldehyde and isobutyraldehyde in the one-pot method under the action of Cu(SbF6)2 and a Pd-ligand catalyst. The one-pot method complies with the characteristics of green chemistry and high atom economy, and significantly reduces the emission of waste water, waste gas, solid waste and pollution factors; has fewer reaction steps and a yield (about 80% to 87%) which is significantly higher than that of the existing multi-step synthesis method technical solutions; has raw materials which are easy to obtain and simple and convenient process operations; has a low risk of EHS; and has high industrial feasibility.
Inventors:
WANG HAIBO (CN)
MEI GUANGYAO (CN)
FANG ZHENRONG (CN)
JIN HUI (CN)
KUANG HONGFU (CN)
ZHANG WEI (CN)
QIU JINFU (CN)
XU CHENLI (CN)
LIU ZHANYU (CN)
LIU XUESHENG (CN)
MEI GUANGYAO (CN)
FANG ZHENRONG (CN)
JIN HUI (CN)
KUANG HONGFU (CN)
ZHANG WEI (CN)
QIU JINFU (CN)
XU CHENLI (CN)
LIU ZHANYU (CN)
LIU XUESHENG (CN)
Application Number:
PCT/CN2020/129673
Publication Date:
March 10, 2022
Filing Date:
November 18, 2020
Export Citation:
Assignee:
ZHEJIANG HONGYUAN PHARMA CO LTD (CN)
International Classes:
C07C231/12; B01J31/22; C07C235/80; C07C239/18; C07D273/04
Domestic Patent References:
| WO2002057274A1 | 2002-07-25 | |||
| WO2012143933A1 | 2012-10-26 | |||
| WO2012143933A1 | 2012-10-26 |
Foreign References:
| US20080280970A1 | 2008-11-13 | |||
| CN202010926970A | 2020-09-07 | |||
| US20040072893A1 | 2004-04-15 |
Other References:
RAO LI , LIU FENG-SI , GUAN SHI-LONG , ZHOU KAI : "Research on the synthesis of 4- (4-Fluorophenyl) -2 (2-Methylpropanoyl) -4-Oxo-N,beta-Diphenylbutanamide", JOURNAL OF WUHAN INSTITUTE OF TECHNOLOGY, vol. 32, no. 12, 15 December 2010 (2010-12-15), pages 10 - 12, XP055837877, ISSN: 1674-2869, DOI: 10.3969/j.issn.1674-2869.2010.12.003
See also references of EP 3984991A4
See also references of EP 3984991A4
Attorney, Agent or Firm:
UNITALEN ATTORNEYS AT LAW (CN)
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