Isonitriles from the Baylis-Hillman adducts of acrylates: viable precursor to tetrazolo-fused diazepinones via post-Ugi cyclization

Stereocontrolled synthesis of substituted isonitriles from the Baylis-Hillman adducts of acrylates has been developed. Ugi reaction of these isonitriles with TMSN3, aliphatic amines, and aldehydes or ketone affords 1-substituted tetrazoles which have been demonstrated to be suitable substrates for producing tetrazolo-fused diazepinones.