Application of 402-46-0, A common heterocyclic compound, 402-46-0, name is 4-Fluorobenzenesulfonamide, molecular formula is C6H6FNO2S, 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.
Example 13; 4-Fluoro-{N-4-[N-(3-fluoro-4-methoxyphenyl)-pyridin-3-ylmethylamino]- benzoyl} benzenesulfonamide; A mixture of 4- [N-(3-fluoro-4-methoxyphenyl)-pyridin-3-ylmethylamino] benzoic acid (50 mg, 0.14 mmol), 4-fluorobenzenesulfonamide (49 mg, 0. 28 mmol), 1- (3-dimethylaminopropyl)-3- ethylcarbodiimide hydrochloride (54 mg, 0.28 mmol), and dimethylaminopyridine (35 mg, 0.28 mmol) was taken up in dichloromethane (1 mL) and stirred for 18h. The mixture was partitioned between EtOAc (50 mL) and 20% aqueous NH40Ac. The EtOAc was separated, washed with brine, dried (MgS04) and concentrated. The residue was purified by column chromatography (silica gel) eluting with 100% EtOAc to give 38 mg of 4-fluoro-f N 4- [N (3-fluoro-4- methoxyphenyl)-pyridin-3-ylmethylamino]-benzoyl} benzenesulfonamide as a white solid. IH NMR (300 MHz, CDC13) 6 8.5-8. 4 (m, 2H), 8. 11 (m, 2H), 7.7-7. 5 (m, 3H), 7.25 (m, 1H), 7.16 (m, 2H), 7.0-6. 8 (m, 3H), 6.63 (d, J=9.0, 2H), 4.92 (s, 2H), 3.89 (s, 3H).
The synthetic route of 402-46-0 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MEMORY PHARMACEUTICALS CORPORATION; WO2005/61458; (2005); A2;,
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