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Convenient synthesis of 1,2,3,4‐tetrahydro‐pyrimidin‐5‐ylbenzoxazoles
Author(s) -
Jung Myung Hee,
Choi SungWon,
Cho KuiWoong
Publication year - 2000
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570370447
Subject(s) - chemistry , iodobenzene , condensation , agonist , combinatorial chemistry , annulation , medicinal chemistry , organic chemistry , catalysis , receptor , biochemistry , physics , thermodynamics
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 M 1 muscarinic agonist candidates.