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Alternative method of Boc-removal from sulfamide using silica-phenyl sulfonic acid in conjunction with microwave heating
Authors:Shahnaz?Ghassemi  author-information"  >  author-information__contact u-icon-before"  >  mailto:sghassemi@biotage.com"   title="  sghassemi@biotage.com"   itemprop="  email"   data-track="  click"   data-track-action="  Email author"   data-track-label="  "  >Email author,Kristin?Fuchs
Affiliation:(1) Biotage, Charlottesville, Virginia, USA;(2) University of Richmond, Virginia, USA
Abstract:Summary A general method was used to prepare an array of unsymmetric sulfamides. This was accomplished by the stepwise addition of CSI to tert-butanol followed by the addition of amines. To increase diversity, nitrogen group of Boc-sulfamides was alkylated with alcohols using Mitsunobu reaction and Boc-group was removed using Si-TsOH. Microwave heating was used in all the steps. The final sulfamides were released from Si-TsOH using NH3 in MeOH.
Keywords:combinatorial library  microwave assisted synthesis  silica-phenyl sulfonic acid  sulfamide
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