Method for high-selectivity synthesis of 3-thio indole

• Main Authors: ZHANG YING, WANG LIXIAN, ZHANG XINGHUA, LU DANNA
• Format: Patent
• Language: Chinese; English
• Published: 26.02.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention relates to a method for high-selectivity synthesis of 3-thio indole, which comprises the following steps: using an indole compound, a sulfonyl hydrazine compound and a bromine source toprepare a mixed solution, adding an oxidant into the mixed solution, and carrying out heating reaction at 60-100 DEG C for 8-10 hours to obtain a crude product; and sequentially carrying out drying, concentration and column chromatography separation on the crude product to obtain the 3-thio indole. Compared with the prior art, the method provided by the invention has the advantages of rapid reaction, high regioselectivity, good substrate expansibility, strong adaptability, simple preparation process, convenient operation and the like, also avoids the use of an organic metal catalyst, reduces the preparation cost, conforms to the environmental protection development concept of green chemistry, and has broad industrial application prospects. 本发明涉及一种高选择性合成3-硫醚吲哚的方法，包括首先将吲哚类化合物、磺酰肼类化合物、溴源配制成混合溶液，再向混合溶液中加入氧化剂，并在60-100℃