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2-{4-[2-methyl-6-(5-phenyl-[1,3,4]oxadiazol-2-ylamino)pyrimidin-4-yl]piperazin-1-yl}ethanol[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
23%
With palladium diacetate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene; sodium t-butanolate; In N,N-dimethyl-formamide; at 110℃; for 36h;Schlenk technique; Inert atmosphere;
General procedure: A 10-ml Schlenk tube equipped with a stir-bar was charged with compound 1 (0.2 mmol), compound 2 (0.3 mmol), Pd(OAc)2 (0.02 mmol), Xantphos (0.04 mmol), NaOtBu (0.3 mmol), anhydrous DMF (2 mL).The reaction tube was purged with argon. The Schlenk tube was placed in an oil-bath at 110 oC for 36 hours and then cooled to room temperature. The reaction mixture was extracted with EtOAc (3 × 20 mL). The combined organic phase was dried over MgSO4 and concentrated under reduced pressure and the crude residue purified by flash chromatography on silica gel. The purified material was dried in vacuo to afford the corresponding products 3a-w.
23%
With xantphos; palladium diacetate; sodium t-butanolate; In N,N-dimethyl-formamide; at 110℃; for 36h;Schlenk technique; Inert atmosphere;
In a 10 ml Schlenk tube, add compound 1c (51.2 mg, 0.2 mmol), 5-phenyl- [1,3,4]oxadiazole-2-amino (48.3 mg, 0.3 mmol), Pd (OAc) 2 (4.5 mg, 0.02 mmol), xantphos (23mg, 0.04mmol), NaOtBu (29mg, 0.3mmol) and anhydrous DMF (2mL) under the protection of argon,The reaction tube was placed in an oil bath at 110 C. for 36 h for a Buchwald-Hartwig reaction, then cooled to room temperature, and the reaction mixture was extracted with EtOAc (3 × 20 mL). The organic phase was dried over MgSO4 and concentrated under reduced pressure. The corresponding product 2a (17.5 mg) was separated on a silica gel column, white solid, melting point: 180 C, yield 23%, purity 96%.
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