Continuous‐Flow Synthesis of (
<i>R</i>
)‐Tamsulosin Utilizing Sequential Heterogeneous Catalysis
作者:Yuki Saito、Ken Nishizawa、Benjamin Laroche、Haruro Ishitani、Shū Kobayashi
DOI:10.1002/anie.202115643
日期:2022.3.21
(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。