【药物名称】Piroxicam, CP-16171, Baxo, Felden, Feldene Fast, Feldene Gel, Feldene
化学结构式(Chemical Structure):
参考文献No.47601
标题:Benzothiazine dioxides
作者:Lombardino, J.G. (Pfizer Inc.)
来源:DE 1943265; FR 2016455; GB 1257180; US 3591584
合成路线图解说明:

The isomerization of methyl 3-oxo-1,2-benzothiazolin-1,1-dioxide-2-acetate (I) by means of sodium methoxide in DMSO gives methyl 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (II), which is methylated with methyl iodide and NaOH in methanol giving methyl 3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (III). Finally, this product is treated with 2-aminopyridine (A) in refluxing xylene.

参考文献No.607582
标题:Sudoxicam and related N.heterocyclic carboxamides of 4-hydroxy-2-methyl-2H-1,2-benzothiazine 1,1-dioxide, potent non steroidal anti-inflammatory agents
作者:Lombardino, J.G.; Wiseman, E.H.
来源:J Med Chem 1972,15(8),848
合成路线图解说明:

The isomerization of methyl 3-oxo-1,2-benzothiazolin-1,1-dioxide-2-acetate (I) by means of sodium methoxide in DMSO gives methyl 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (II), which is methylated with methyl iodide and NaOH in methanol giving methyl 3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (III). Finally, this product is treated with 2-aminopyridine (A) in refluxing xylene.

参考文献No.607782
标题:Potent anti-inflammatory N-heterocyclic 3-carboxamides of 4-hydroxy-2-methyl-2H-1,2-benzothiazine 1,1-dioxide
作者:Lombardino, J.G.; Wiseman, E.H.; Chiaini, J.
来源:J Med Chem 1973,16(5),493
合成路线图解说明:

The isomerization of methyl 3-oxo-1,2-benzothiazolin-1,1-dioxide-2-acetate (I) by means of sodium methoxide in DMSO gives methyl 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (II), which is methylated with methyl iodide and NaOH in methanol giving methyl 3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (III). Finally, this product is treated with 2-aminopyridine (A) in refluxing xylene.

参考文献No.800628
标题:Piroxicam
作者:Arrigoni-Martelli, E.; Casta馿r, J.
来源:Drugs Fut 1977,2(2),124
合成路线图解说明:

The isomerization of methyl 3-oxo-1,2-benzothiazolin-1,1-dioxide-2-acetate (I) by means of sodium methoxide in DMSO gives methyl 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (II), which is methylated with methyl iodide and NaOH in methanol giving methyl 3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-1,1-dioxide-3-carboxylate (III). Finally, this product is treated with 2-aminopyridine (A) in refluxing xylene.

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