Synthetic Route of 39806-90-1, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 39806-90-1, name is 4-Iodo-1-methyl-1H-pyrazole, This compound has unique chemical properties. The synthetic route is as follows.
To a solution of 4-iodo-l-methyl-lH-pyrazole (20.14 mg, 0.097 mmol) in anhydrous DMSO (5 ml) was added intermediate 20.1-2 (20 mg, 0.065 mmol), (iras,)-Nl,N2-dimethylcyclohexane- 1, 2-diamine (1.837 mg, 0.013 mmol), potassium phosphate (41.1 mg, 0.194 mmol) and Cul (1.230 mg, 6.46 pmol). The resulting mixture was stirred at 90C under N2 protection for 12 hours. After filtration and concentration, the crude product was purified by pre-HPLC (TFA) to give example 20.2-2, ( R,R or .V,.Y)-5-chloro-6-(3-nuoro- 1 -(oetan-3-yl)piperidin-4-yl)- 1 -( 1 -methyl- 1 H-pyra/ol- 4-yl)-lH-indazole, TFA salt. MS (ESI) m/z calc?d for C19H22CIFN5O [M+H]+ 390, found 390. NMR (400 MHz, CD3OD) d 8.27 (s, 1H), 8.17 (s, 1H), 7.95 (s, 1H), 7.89 (s, 1H), 7.65-7.85 (m, 1H), 5.39-5.62 (m, 1H), 5.39-5.62 (m, 1H), 4.95-5.05 (m, 4H), 4.59 (m, 1H), 4.02 (s, 3H), 3.81- 4.00 (m, 2H), 3.56 (m, 1H), 3.11-3.26 (m, 2H), 2.20-2.37 (m, 2H). LRRK2 IC50 5.8 nM.
The chemical industry reduces the impact on the environment during synthesis 4-Iodo-1-methyl-1H-pyrazole. I believe this compound will play a more active role in future production and life.
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;,
Pyrazole – Wikipedia,
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