625470-36-2Relevant articles and documents
3-cyclopropyl benzenesulfonyl benzylamine and synthesis method thereof
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Paragraph 0010-0013; 0018-0021, (2020/05/05)
The invention relates to a 3-cyclopropyl benzenesulfonyl benzylamine and a synthesis method therepf, the preparation method comprises the following steps: dissolving 3-bromobenzenesulfonic acid and benzylamine in pyridine, then adding a condensing agent EDC-HCl, and carrying out a reaction for 2 to 3 h at a temperature of 50 to 80 DEG C so as to obtain 3-bromo-N-benzylbenzenesulfonamide; dissolving 3-bromo-N-benzylbenzenesulfonamide into a dioxane solution; adding cyclopropylboronic acid, sodium carbonate, water and Pd(dppf) Cl2, reacting a mixed system in a nitrogen atmosphere at 110 DEG C for 8-10 hours, and carrying out post-treatment to obtain the 3-cyclopropylbenzenesulfonyl benzylamine. The preparation method has the advantages of relatively mild conditions, easy treatment and purification of the product, and suitability for batch preparation.
Methylprenyl and prenyl protection for sulfonamides
Nikitjuka, Anna,Nekrasova, Aleksandra,Jirgensons, Aigars
, (2015/02/02)
2-Methylprenyl (MePre) is an efficient protection for sulfonamides. The acidic cleavage of this group leads to volatile by-products and the product can be obtained in high purity without additional purification. MePre group is resistant to Pd/C-catalysed hydrogenolysis at 1 atm, Suzuki-Miyaura reaction, Ni(0) catalysis conditions and oxidising reagents such as NIS and DDQ. The prenyl (Pre) group can also be used to protect sulfonamides in certain cases; however, the substrate scope is limited due to the side product formation.