With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1242156-59-7,6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one,as a common compound, the synthetic route is as follows.
Step 5. Preparation of 2-(6-tert-butyl-8-fluoro-l-oxo-lH-phthalazin-2-yl)-4-iodo-pyridine-3- carbaldehyde Method A In a 1 L round-bottomed flask, 6-tert-butyl-8-fluorophthalazin-l(2H)-one (5.6 g, 25.4 mmol) was combined with THF (300 ml) to give a colorless solution. Sodium hydride (1.12 g, 28.0 mmol) was added. The reaction mixture was stirred at ambient temperature for 10 min. 2-Fluoro-4- iodonicotinaldehyde (7.02 g, 28.0 mmol) was added and the reaction mixture was stirred at ambient temperature for 1 h. The reaction was complete as determined by LCMS analysis. The reaction mixture was quenched with saturated NH4CI. The reaction mixture was poured into 200 mL of H20 and extracted thrice with CH2CI2. The organic layers were washed with brine, then dried over Na2S04 and concentrated under vacuum. The resultant bright yellow solid was transferred into a filter funnel and the flask washed twice with a small volume of EtOAc to ensure complete transfer of the solid into the funnel. The liquid was filtered through. The solid was triturated twice with Et20 and dried under vacuum to afford the desired product as a cream- colored solid (8.09 g, 17.9 mmol, 70.5 % yield). (M+H)+ = 452 m/e. *H NMR (400 MHz, CUC -d) delta ppm 1.44 (s, 9 H) 7.49 – 7.54 (m, 1 H) 7.54 (d, 7=1.77 Hz, 1 H) 8.03 (d, 7=5.31 Hz, 1 H) 8.30 (d, 7=2.53 Hz, 1 H) 8.37 (d, 7=5.31 Hz, 1 H) 9.98 (s, 1 H)., 1242156-59-7
The synthetic route of 1242156-59-7 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; IYER, Raman Mahadevan; LAINE, Dramane Ibrahim; LOPEZ-TAPIA, Francisco Javier; PHILLIPS, Jonathan E.; STEVENSON, Christopher; WO2014/83026; (2014); A1;,
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