Reference of 5071-61-4, These common heterocyclic compound, 5071-61-4, name is 5-Phenyl-1H-pyrazole-3-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.
Step 2B: Synthesis of l-(5-phenyl-lH-pyrazole-3-carbonyl)-N-(pyrimidin-2-yl)- N-{[2-(trimethylsilyl)ethoxy]methyl}-2,3-dihydro-lH-indole-5-sulfonamide 37.1 [00464] DIPEA (0.16 ml, 0.89 mmol) and HATU (170mg, 0.45 mmol) were added at rt to a stirred solution of 5 -phenyl- lH-pyrazole-3-carboxylic acid (60mg, 0.30 mmol) in DMF (HPLC grade, 10ml) followed by N-(pyrimidin-2-yl)-N-{[2-(trimethylsilyl)ethoxy]methyl}-2,3-dihydro- lH-indole-5 -sulfonamide (34.1, 120mg, 0.30 mmol). The mixture was stirred for 27h at rt then re-treated with 5 -phenyl- lH-pyrazole-3-carboxylic acid (30mg, 0.15 mmol), DIPEA (0.20 ml, 1.1 mmol) and HATU (220mg, 0.58 mmol) and stirred for 74h at rt. The solvent was removed in vacuo and the crude product purified by prep HPLC (MeCN/Water, 2mM ammonium bicarbonate) to afford 46mg (27%) of 1 -(5 -phenyl- lH-pyrazole-3 -carbonyl)-N-(pyrimidin-2-yl)- N-{[2-(trimethylsilyl)ethoxy]methyl}-2,3-dihydro-lH-indole-5-sulfonamide 37.1 as an off-white solid.
The synthetic route of 5071-61-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; RAZE THERAPEUTICS, INC.; SAIAH, Eddine; (148 pag.)WO2016/40449; (2016); A1;,
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