- 专利标题: Synthesis of 6-aryl-4-aminopicolinates and 2-aryl-6-aminopyrimidine-4-carboxylates by direct suzuki coupling
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申请号: US16045896申请日: 2018-07-26
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公开(公告)号: US10544121B2公开(公告)日: 2020-01-28
- 发明人: Jason S. Fisk , Xiaoyong Li , Mark Muehlfeld , Robert S. Bauman , Jossian Oppenheimer , Siyu Tu , Mark A. Nitz , Reetam Chakrabarti , Shawn D. Feist , James W. Ringer , Ronald B. Leng
- 申请人: Dow AgroSciences LLC
- 申请人地址: US IN Indianapolis
- 专利权人: Dow AgroSciences LLC
- 当前专利权人: Dow AgroSciences LLC
- 当前专利权人地址: US IN Indianapolis
- 主分类号: C07D401/04
- IPC分类号: C07D401/04 ; B01J31/00 ; B01J35/00 ; C07D213/79 ; C07D213/90 ; C07D239/02 ; C07D239/28 ; C07D239/32
摘要:
Improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates and arylalkyl and alkyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates, are described herein. The improved methods include a direct Suzuki coupling step, which eliminates the protection/de-protection steps in the current chemical process, and therefore eliminates or reduces various raw materials, equipment and cycle time as well as modification of other process conditions including use of crude AP, use of ABA-diMe, and varying pH, catalyst concentration, solvent composition, and/or workup procedures. This includes synthesis of 2-aryl-6-aminopyrimidine-4-carboxylates.
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