CAS: 163457-23-6; 3,3-Difluoropyrrolidine Hydrochloride

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CAS号195447-25-7 1-B°C-3,3-二氟吡咯烷 | CAS号877125-71-8 4-(3,3-二氟吡咯烷-1-...

3,3-二氟吡咯烷丁-2-酮置于硼烷四氢呋喃络合物,甲醇,盐酸体系中,用 四氢呋喃,1,4-二氧六环 用作溶剂,化学反应 5.0H,以82%的收率获得3,3-二氟吡咯烷盐酸
参考文献:从2-氯-2,2-二氟乙酸开始的3,3-二氟吡咯烷盐酸盐的有效合成
标题:从2-氯-2,2-二氟乙酸开始的3,3-二氟吡咯烷盐酸盐的有效合成
摘要:据报道,3,3-二氟吡咯烷盐酸盐(3)的合成简便,无氟化,是生物活性化合物合成中的重要合成子.七步合成过程从市售的2-氯-2,2-二氟乙酸(1)开始,分三步伸缩,生成晶体n,N-N-二乙基-2,2-二氟-3-羟基-4-硝基丁酰胺(2).方便且高产的2的还原硝基甲基化,然后进行催化的加氢/环化顺序和硼烷还原,可得到3的高收率和纯度.
Doi:10.1016/j.Jfluchem.2011.08.009

专利信息

专利号:US-9428490-B2
优先权日:2011-07-29
标 题 :Nuclear transport modulators and uses thereof
发明人：SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD
权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD; KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

专利号:US-9957277-B2
优先权日:2015-11-25
标题 :eIF4A-inhibiting compounds and methods related thereto
发明人：ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; TRAN CHINH VIET; PACKARD Garrick Kenneth; XIANG ALAN X; NILEWSKI CHRISTIAN; MICHELS THEO
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds X, Y, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b and R 5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.