新型C2-芳基吡咯并[2,1-c][1,4]苯并二氮杂䓬（PBD）文库的平行合成
Parallel synthesis of a novel C2-aryl pyrrolo[2,1-c][1,4]benzodiazepine (PBD) library.
作者信息
Antonow Dyeison, Cooper Nectaroula, Howard Philip W, Thurston David E
机构信息
Spirogen Limited, 2 Royal College Street, London NW1 0NH, UK.
出版信息
J Comb Chem. 2007 May-Jun;9(3):437-45. doi: 10.1021/cc0601332. Epub 2007 Mar 31.
PMID:17397227
Abstract
A 66-member C2-aryl pyrrolo[2,1-c][1,4]benzodiazepine (PBD) library has been successfully synthesized in parallel via Suzuki coupling using PS-PPh3Pd (catalyst) and PS-DEAM (scavenger) under microwave radiation. Library members were obtained in sufficient yield (up to 91%) and purity (85-98% crude) for biological evaluation.
摘要
通过在微波辐射下使用PS-PPh3Pd（催化剂）和PS-DEAM（清除剂）进行铃木耦合反应，成功地并行合成了一个由66个成员组成的C2-芳基吡咯并[2,1-c][1,4]苯并二氮杂卓（PBD）文库。文库成员的产率足够高（高达91%），纯度也足以用于生物学评估（粗品纯度为85-98%）。
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