浙江化工
浙江化工
절강화공
Zhejiang Chemical Industry
2015年
9期
1-2
,共2页
(1R,2S)-2-(3,4-二氟苯基)环丙胺D-扁桃酸盐%替卡格雷%中间体%合成
(1R,2S)-2-(3,4-二氟苯基)環丙胺D-扁桃痠鹽%替卡格雷%中間體%閤成
(1R,2S)-2-(3,4-이불분기)배병알D-편도산염%체잡격뢰%중간체%합성
(1R,2S)-2-(3,4-difluorophenyl)cyclopropylamine mandelate%ticagrelor%intermediate%synthe-sis
以邻二氟苯为原料，经傅克酰化、缩合、还原、环合，最后与D-扁桃酸成盐制得替卡格雷关键中间体(1R,2S）-2-(3,4-二氟苯基）环丙胺扁桃酸盐，总收率32.6%，ee值99.8%。
以鄰二氟苯為原料，經傅剋酰化、縮閤、還原、環閤，最後與D-扁桃痠成鹽製得替卡格雷關鍵中間體(1R,2S）-2-(3,4-二氟苯基）環丙胺扁桃痠鹽，總收率32.6%，ee值99.8%。
이린이불분위원료，경부극선화、축합、환원、배합，최후여D-편도산성염제득체잡격뢰관건중간체(1R,2S）-2-(3,4-이불분기）배병알편도산염，총수솔32.6%，ee치99.8%。
(1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamine mandelate,the key intermediate of ticagrelor, was synthesized form 1,2-difluorobenzene via Friedel-Crafts acylation,condensation, recovery, cyclization with a yield of 32.6%. The ee value of the target compound was 99.8%.
