(R)-tamsulosin, three C−N bond formation/cleavage reactions with hydrogen gas over heterogeneous catalysts enabled the efficient construction of the key skeleton. Two different polysilane-modified Pd catalysts were developed for these transformations, which were followed by a deprotection step under homogeneous catalysis to provide tamsulosin in 60 % overall yield in a flow stream.
在
(R)-坦洛新的多步连续流合成中,在非均相催化剂上与
氢气的三个 C-N 键形成/裂解反应能够有效构建关键骨架。为这些转化开发了两种不同的聚
硅烷改性的 Pd 催化剂,然后在均相催化下进行脱保护步骤,从而以 60% 的总收率在流动流中提供
坦洛新。