Department of Chemistry, The University of Texas at San Antonio, San Antonio, Texas 78249, United States.
Chemical Process Development, Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08901, United States.
Org Lett. 2021 May 7;23(9):3233-3236. doi: 10.1021/acs.orglett.1c00179. Epub 2021 Feb 25.
A simple metal-free method has been developed for the reductive N-alkylation of indoles employing aldehydes as the alkylating agent and inexpensive EtSiH as the reductant. A wide range of aromatic and aliphatic aldehydes are viable substrates along with a variety of substituted indoles. In addition, the method was applied to a one-pot sequential 1,3-alkylation of a substituted indole and successfully demonstrated on a 100 mmol scale.
一种简单的无金属方法已经被开发出来，用于吲哚的还原 N-烷基化，使用醛作为烷基化试剂，廉价的 EtSiH 作为还原剂。各种芳香醛和脂肪醛都是可行的底物，还有各种取代的吲哚。此外，该方法还被应用于取代吲哚的一锅法连续 1,3-烷基化，并在 100mmol 规模上成功得到了验证。
