Reference of 1239363-40-6,Some common heterocyclic compound, 1239363-40-6, name is 1-Cyclopropyl-4-iodo-1H-pyrazole, molecular formula is C6H7IN2, 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.
To a solution of potassium phosphate tribasic (792 mg, 3.73 mmol) and l-cyclopropyl-4-iodo-lH- pyrazole (437 mg, 1.866 mmol) in DMSO (10 mL) were added intermediate 41.4 (530 mg, 1.244 mmol), Irans-N 1.N2-dimethylcycloheane- 1.2-diamine (35.4 mg, 0.249 mmol) and copper(I) iodide (237 mg, 1.244 mmol) at room temperature. The mixture was stirred for 36 h at 90C under N2 atmosphere. 16% NEL aqueous (20 mL) was added to the mixture and this mixture was extracted with EtOAc (10 mL x 3). The combined organic layers were washed with brine (20 mL), dried over Na2S04 and filtered. The filtrate was concentrated in vacuo to give intermediate 41.5, 6-(l-(4-(benzyloxy)-3-methyltetrahydrofuran-3-yl)piperidin-4-yl)-5-chloro-l-(l-cyclopropyl- lH-pyrazol-4-yl)-lH-indazole. MS (ESI) m/z calc?d for C30H35CIN5O2 [M+H] + 532 found 532.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1-Cyclopropyl-4-iodo-1H-pyrazole, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; SIMOV, Vladimir; KAPLAN, William, P.; ACTON, John, J., III; ARDOLINO, Michael, J.; CHEN, Joanna, L.; FULLER, Peter, H.; GUNAYDIN, Hakan; LI, Derun; LIU, Ping; LOGAN, Kaitlyn Marie; METHOT, Joey; MORRIELLO, Gregori, J.; NEELAMKAVIL, Santhosh, F.; TORRES, Luis; YAN, Xin; ZHOU, Hua; (0 pag.)WO2020/92136; (2020); A1;,
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