Advanced Synthesis & Catalysis

Catalytic Asymmetric Total Synthesis of the Muscarinic Receptor Antagonist (R)??Tolterodine

C Hedberg, PG Andersson

Index: Hedberg, Christian; Andersson, Pher G. Advanced Synthesis and Catalysis, 2005 , vol. 347, # 5 p. 662 - 666

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Citation Number: 30

Abstract

Abstract A convenient and high yielding method for the preparation of (R)-tolterodine, utilizing a catalytic asymmetric Me-CBS reduction was developed. Highly enantioenriched (R)-6-methyl-4-phenyl-3, 4-dihydrochromen-2-one (94% ee) was recrystallized to yield practically enantiopure material (ee> 99%) and converted to (R)-tolterodine in a four-step procedure. The configuration of the crucial stereocenter was preserved during the ...