【药物名称】Amlexanox, Amoxanox, CHX-3673, AA-673, OraDisc A, Aptheal, Apthera, OraRinse, Aphthasol, Elics, Solfa
化学结构式(Chemical Structure):
参考文献No.46462
标题:1-Azaxanthone-3-carboxylic acid
作者:Nohara, A.; Sugihara, H.; Ukawa, K. (Takeda Chemical Industries, Ltd.)
来源:BE 0864647; DE 2809720; FR 2383185; GB 1597024; GB 1597025; JP 78111096; JP 78111097; JP 7988298; US 4143042; US 4255576; US 4299963
合成路线图解说明:

The reaction of 6-isopropyl-4-oxo-4H-1-benzopyran-3-carbonitrile (I) with morpholine (A) and DMF in hot water gives 2-amino-6-isopropyl-4-oxo-4H-1-benzopyran-3-carboxaldehyde (II), which is cyclized with ethyl cyanoacetate (III) by means of piperidine (B) in refluxing ethanol yielding ethyl 2-amino-7-isopropyl-1-azaxanthone-3-carboxylate (IV). Finally, this compound is saponified by a treatment with sulfuric acid in refluxing acetic acid water.

参考文献No.49360
标题:AA-673
作者:Serradell, M.N.; Casta馿r, J.
来源:Drugs Fut 1984,9(5),311
合成路线图解说明:

The reaction of 6-isopropyl-4-oxo-4H-1-benzopyran-3-carbonitrile (I) with morpholine (A) and DMF in hot water gives 2-amino-6-isopropyl-4-oxo-4H-1-benzopyran-3-carboxaldehyde (II), which is cyclized with ethyl cyanoacetate (III) by means of piperidine (B) in refluxing ethanol yielding ethyl 2-amino-7-isopropyl-1-azaxanthone-3-carboxylate (IV). Finally, this compound is saponified by a treatment with sulfuric acid in refluxing acetic acid water.

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