A common heterocyclic compound, 272437-84-0,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route. 272437-84-0
272437-84-0, Preparation of 3-oxo-3,4-dihvdro-2H-benzori,41thiazine-6-carboxylic acid (l-[2-(7- methoxy-quinoxalin-2-ylsulfanyl)-ethvH-piperidin-4-vU -methyl-amide: 3-oxo-3,4-dihydro-2H-benzo[l,4]thiazine-6-carboxylic acid (26 mg, 0.11 mmol, 1.0 eq) is added at room temperature to a stirred solution of {l-[2-(7-methoxy-quinoxalin-2- ylsulfanyl)-ethyl]-piperidin-4-yl}-methyl-amine (40 mg, 0.11 mmol, 1.0 eq) in N,N- dimethylformamide (3 mL), followed by O-(7-azabenzotriazol-l-yl)-iV,iV,N’,N’- tetramethyluronium hexafluorophosphate (45 mg, 0.11 mmol, 1.0 eq), and triethylamine (16 muL, 0.11 mmol, 1.0 eq). After 4 hours stirring at room temperature, solvent is evaporated and the residue is purified by preparative EtaPLC to afford 3-oxo-3,4-dihydro-2H- benzo[l,4]thiazine-6-carboxylic acid {l-[2-(7-methoxy-quinoxalin-2-ylsulfanyl)-ethyl]- piperidin-4-yl} -methyl-amide as a yellow solid (22 mg, 35% yield).MS m/z (+ESI): 524.3 [M+Eta]”
This compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid,272437-84-0,its application will become more common.
Reference£º
Patent; BASILEA PHARMACEUTICA AG; GAUCHER, Berangere; DANEL, Franck Hubert; ROUSSEL, Patrick; WO2010/84152; (2010); A1;,
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