Related Products of 4522-35-4, These common heterocyclic compound, 4522-35-4, name is 3-Iodo-1H-pyrazole, 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.
INTERMEDIATE 22 4-(3-Iodo-lH-pyrazol-l-yl -N7V-dimethylpyridin-2-amine To a suspension of 3-iodo-lH-pyrazole (100 mg, 0.516 mmol) and N,N-dimethyl-4- (4,4,5, 5-tetramethyl-l,3,2-dioxaborolan-2-yl)pyridin-2-amine (1 2 mg, 0.773 mmol), Na2C03 (109 mg, 1.031 mmol) in anhydrous dichloroethane (4 mL) added a suspension of Cu(OAc)2 (94 mg, 0.516 mmol) and 2,2′-bipyridine (81 mg, 0.516 mmol) in dichloroethane (4 mL). The reaction was stirred at 70 C under N2 overnight. The mixture was filtered through the Celite and washed with EtOAc (5 mL x 3), the filtrate was collected and removed in vacuo to give the crude product. This was purified by flash chromatography (ISCO Combiflash, lOg, Biotage Si column, -30 mL/min, 100% hexanes 5 min, gradient to 100% EtOAc in hexanes 15 min) to afford 4-(3-iodo-lH-pyrazol-l-yl)-N,N-dimethylpyridin-2-amine. LCMS calc. = 315.01 ; found = 315.10 (M+H)+.
The synthetic route of 4522-35-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK SHARP & DOHME CORP.; MOCHIDA PHARMACEUTICAL CO., LTD.; SMITH, Cameron, James; TAN, John, Qiang; ZHANG, Ting; BALKOVEC, James; GREENLEE, William, John; GUO, Liangqin; XU, Jiayi; CHEN, Yi-heng; CHEN, Yili; CHACKALAMANNIL, Samuel; HIRABAYASHI, Tomokazu; NAGASUE, Hiroshi; OGAWA, Kouki; WO2014/120346; (2014); A1;,
Pyrazole – Wikipedia,
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