摘要 一个简单而有效的合成2-芳基-3-羟基噻吩并[3,2- b ]吡啶-7(4 H)-ones,7-甲氧基-2,3-二芳基噻吩并[3,2- b ]吡啶和2提出了,3-二芳基噻吩并[3,2- b ]吡啶-7(4 H)-one。合成包括在3位上对4-甲氧基吡啶甲酸甲酯进行硫代烷基化,然后原位环化,得到2-芳基-7-甲氧基噻吩并[3,2 - b ]吡啶-3-醇。这些化合物的脱甲基得到相应的2-芳基噻吩并[3,2 - b ]吡啶-7(4 H)-。7-甲氧基-2-芳基噻吩并[3,2- b]的进一步功能化通过将羟基转化为相应的三氟甲磺酸酯来获得]吡啶-3-醇,然后将其进行钯催化的交叉偶联,得到7-甲氧基-2,3-二(杂)芳基噻吩并[3,2- b ]吡啶。随后7-甲氧基的去甲基化得到相应的吡啶酮。 一个简单而有效的合成2-芳基-3-羟基噻吩并[3,2- b ]吡啶-7(4 H)-ones,7-甲氧基-2
A novel one-pot synthesis of 7-methoxy-2-arylthieno[3,2-b]pyridine-3-ols in domino fashion
摘要:
A simple and efficient synthesis of 7-methoxy-2-arylthieno[3,2-b]pyridine-3-ols was achieved using a novel one-pot LDA-promoted domino reaction. Although this class of compounds are not very well represented in the literature, similar skeletons are of immense biological importance. A few closely related compounds are reported with multi-step syntheses using harsh conditions and longer reaction time. (C) 2013 Elsevier Ltd. All rights reserved.