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Pictet-Spengler Reaction for the Synthesis of Tetrahydroisoquinolines and Related Heterocyclic Compounds
Pictet-Spengler Reaction for the Synthesis of Tetrahydroisoquinolines and Related Heterocyclic Compounds
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机译:Pictet-Spengler反应用于合成四氢异喹啉和相关杂环化合物
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摘要
A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
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