Abstract
Trimethylsilyl triflate (TMSOTf) can be efficiently used for the synthesis of isochromans via Pictet–Spengler type reaction of vinylogous esters in good yields. The methodology is applied for the formal synthesis of key intermediate alcohols for the synthesis of D 4 antagonist sonepiprazole (±)-U-101387 and the isochroman (±)-U-54537.
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