A formal synthesis of a muscarinic M_1 receptor antagonist,(-)-tan1251a

摘要

An aromatic oxidation reaction of a secondary amine,prepared from L-tyrosine and glycine,with hypervalent iodine reagent gave a spirocyclic product,which was further converted into the key intermediate for the synthesis of (-)-tan1251A.Tan1251a(1),b(2),c(3)and d(4),having unique structural features with a 1,4-diazabicyclo[3.2.1]octane ring system and a spirocyclic cyclohexanone,were isolated from a penicillum thomii R89 by Takeda Industries (Figure 1)~1.