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METHOD FOR DEPROTECTING ARYL OR ALKYL SULFONAMIDES OF PRIMARY OR SECONDARY AMINES

机译:初级或二级胺的芳烷基或烷基磺酰胺的保护方法

摘要

The invention relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by contacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal - silica gel material in the presence of a solid proton source under conditions sufficient to form the corresponding amine. The invention also relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by a) reacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal - silica gel material, and b) subsequently reacting the reaction product from step a) with an electrophile or a proton source. Preferred Stage 0 or Stage I alkali metal - silica gel materials include Na, K2Na, and Na2K.
机译:本发明涉及一种通过在固体存在下使烷基磺酰胺或芳基磺酰胺与阶段0或阶段I碱金属-硅胶材料接触而从伯胺或仲胺中去除烷基磺酰基或芳基磺酰基保护基的方法。质子源在足以形成相应胺的条件下。本发明还涉及通过以下方式从伯胺或仲胺除去烷基磺酰基或芳基磺酰基保护基的方法:a)使烷基磺酰胺或芳基磺酰胺与第0级或第I级碱金属-硅胶材料反应,和b )随后使步骤a)的反应产物与亲电试剂或质子源反应。优选的阶段0或阶段I的碱金属-硅胶材料包括Na,K 2 Na和Na 2K。

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