Title:
DIFLUOROMETHYLATION AGENT, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/047985
Kind Code:
A1
Abstract:
The present invention belongs to the technical field of chemical preparation, and particularly relates to a difluoromethylation agent, preparation therefor and use thereof. Aiming at the key problem of poor stability of current electrophilic difluoromethylation agents, the problem of agent stability is solved by means of innovative design. An electrophilic difluoromethylation agent stably stored at room temperature is synthesized. The difluoromethylation agent can satisfy the difluoromethyl functionalization of different types of substrates, and can be used to develop a variety of new methods and reactions for difluoromethylation. Furthermore, the agent is a solid, easy to use, and highly operable.
Inventors:
LIU GUOKAI (CN)
LU SHENGLE (CN)
LI XIN (CN)
QIN WENBING (CN)
LU SHENGLE (CN)
LI XIN (CN)
QIN WENBING (CN)
Application Number:
PCT/CN2018/113547
Publication Date:
March 12, 2020
Filing Date:
November 02, 2018
Export Citation:
Assignee:
UNIV SHENZHEN (CN)
International Classes:
C07C323/17; C07C17/26; C07C23/36; C07C319/14; C07C319/20; C07C323/18; C07C323/21
Foreign References:
| CN101674826A | 2010-03-17 | |||
| CN107235878A | 2017-10-10 |
Other References:
LU , SHENGLE ET AL.: "Air and Light-Stable S-(Difluoromethyl)sulfonium Salts: C-Selective Electrophilic Difluoromethylation of (3-Ketoesters and Malonates", ORGANIC LETTERS, vol. 20, no. 21, 12 October 2018 (2018-10-12), pages 6925 - 6929, XP055690454, ISSN: 1523-7052
LIU, GUOKAI ET AL.: "Efficient Difluoromethylation of Sp3 Carbon Nucleophiles by Bromodifluoromethylation Reagents with Organic Bases", CHEMISTRYOPEN, vol. 1, no. 5, 31 December 2012 (2012-12-31), pages 227 - 231, XP055690457, ISSN: 2191-1363
PRAKASH, G.K.S. ET AL.: "Direct Electrophilic Monofluoromethylation", ORGANIC LETTERS, vol. 10, no. 4, 17 January 2008 (2008-01-17), pages 557 - 560, XP002660281, ISSN: 1523-7060, DOI: 10.1021/ol702500u
WEB, YING ET AL.: "Effects of 7-methoxy-1-tetralone on the proliferation, apoptosis, migration of HepG2 in human liver cancer and its immunological effects", GUANGDONG MEDICAL JOURNAL, vol. 37, no. 13, 31 July 2016 (2016-07-31), pages 1937 - 1943, ISSN: 1001-9448
LIU, GUOKAI ET AL.: "Efficient Difluoromethylation of Sp3 Carbon Nucleophiles by Bromodifluoromethylation Reagents with Organic Bases", CHEMISTRYOPEN, vol. 1, no. 5, 31 December 2012 (2012-12-31), pages 227 - 231, XP055690457, ISSN: 2191-1363
PRAKASH, G.K.S. ET AL.: "Direct Electrophilic Monofluoromethylation", ORGANIC LETTERS, vol. 10, no. 4, 17 January 2008 (2008-01-17), pages 557 - 560, XP002660281, ISSN: 1523-7060, DOI: 10.1021/ol702500u
WEB, YING ET AL.: "Effects of 7-methoxy-1-tetralone on the proliferation, apoptosis, migration of HepG2 in human liver cancer and its immunological effects", GUANGDONG MEDICAL JOURNAL, vol. 37, no. 13, 31 July 2016 (2016-07-31), pages 1937 - 1943, ISSN: 1001-9448
Attorney, Agent or Firm:
SHENZHEN LAN FENG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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