Convenient synthesis of 1,2,3,4‐tetrahydro‐pyrimidin‐5‐ylbenzoxazoles

2‐Pyrimidin‐5‐ylbenzoxazoles 7 have been synthesized by condensation of 5‐pyrimidinecarboxaldehyde 4 with substituted aminophenols 5 followed by oxidative cyclization of the resulting Schiff's bases 6 with iodobenzene diacetate. Subsequent formation of methylpyrimidinium salts 8 and reduction thereafter afforded tetrahydropyrimidinylbenzoxazoles 10. This method has been utilized in the synthesis of M₁ muscarinic agonist candidates.