<scp>Cu‐Catalyzed</scp>
Chemoselective Reduction of
<scp>
<i>N</i>
‐Heteroaromatics
</scp>
with
<scp>
NH
<sub>3</sub>
</scp>
·
<scp>
BH
<sub>3</sub>
</scp>
in Aqueous Solution
作者:Chao Gao、Qingqing Xuan、Qiuling Song
DOI:10.1002/cjoc.202100259
日期:2021.9
An efficient catalytic system was successfully developed on reduction of N-heteroaromatics with H3N∙BH3 as hydrogen source in CuSO4 solution, featuring excellent chemoselectivity as well as very broad functional group tolerance. Various challenging substrates, such as OH-, NH2-, Cl-, Br-, etc., contained quinolines, quinoxalines, 1,5-naphthyridines and quinazolines were all reduced smoothly. Mechanistic
The invention relates to compound of the formula I
in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.