28395-11-1Relevant articles and documents
Synthesis method of intermediate of bumetanib
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, (2021/12/07)
The invention discloses a synthesis method of an intermediate of bumetanib. The comprises the following steps: protecting amino in 3-amino-4-chlorobenzoic acid as shown in a formula 1 by using a compound containing a benzyl protecting group to obtain a compound as shown in a formula 2; reacting the compound as shown in the formula 2 with thionyl chloride, and treating with ammonia water to obtain a compound as shown in a formula 3; reacting the compound as shown in the formula 3 with phenol to obtain a compound as shown in a formula 4; and reacting the compound as shown in the formula 4 with an oxidizing agent to obtain a bumetanib intermediate as shown in a formula 5, namely 3-amino-4-phenoxy-5-sulfamoyl benzoic acid. Compared with the prior art, the method provided by the invention has the advantages that the use of highly toxic chlorosulfonic acid is avoided, the nitration reaction is avoided, the production organization is facilitated, and the production safety is improved.
Process for the manufacture of substituted amino-benzoic acid derivatives
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, (2008/06/13)
3-Alkylamino-5-sulfamyl benzoic acid derivatives are prepared by reducing 3-acylamino-5-sulfamyl-benzoic acid derivatives by means of boron hydrides or complex boron hydrides in the presence of Lewis acids.