Synthetic method of high-region and high-stereoselectivity-4-alkyl-4-amino-2-fluoro-2-butenoic acid ester

• Main Authors: MA YUFAN, LIN YUN
• Format: Patent
• Language: Chinese; English
• Published: 27.09.2022
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a (Z)-4-alkyl-4-amino-2-fluoro-2-butenoic acid ester compound and a synthetic method for defluorination and amination with high area and high stereoselectivity under the catalysis of metal palladium, and a preparation method of the (Z)-4-alkyl-4-amino-2-fluoro-2-butenoic acid ester compound. The structure of the compound is shown as a formula (1), wherein a substituent group R1 is alkyl or aryl, R2 is H, alkyl or aryl, R3 is alkyl or aryl, or R2R3 is connected into a ring. The method disclosed by the invention is simple and convenient, mild in condition, good in substrate universality, good in yield and high in regioselectivity, the yield of a target object can reach 42%-91%, an amination reaction selectively occurs at the 4-site of the substrate, a defluorination reaction is performed at the same time, and the Z-configuration monofluoroalkenyl carboxylic ester compound is synthesized with high stereoselectivity. 本发明公开了一种(Z)-4-烃基-4-氨基-2-氟-2-丁烯酸酯类化合物和金属钯催化的高区域和高立体选择性的脱氟氨基化的合成方法。所述化合物的结构