Synthesis of functionalised sulfonamides via microwave assisted displacement of PFP-sulfonates with amines

被引:14
作者
Caddick, S
Wilden, JD
Bush, HD
Judd, DB
机构
[1] UCL, Christopher Ingold Labs, Dept Chem, London WC1H 0AJ, England
[2] GlaxoSmithKline Inc, Harlow CM20 2QR, Essex, England
来源
QSAR & COMBINATORIAL SCIENCE | 2004年 / 23卷 / 10期
关键词
D O I
10.1002/qsar.200420038
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A convenient microwave assisted synthesis of sulfonamides from PFP-sulfonates is described. Reaction of various commercially available amines with pentafluorophenyl (PFP) sulfonate esters under microwave irradiation led to the corresponding sulfonamide products in good yields and without the requirement for chromatographic purification. The data shows that a number of functional groups are tolerated in both the amine and sulfonate ester and that the method can be extended to heterocyclic sulfonamides of potential biological interest.
引用
收藏
页码:902 / 905
页数:4
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