Synthetic Route of 120781-02-4,Some common heterocyclic compound, 120781-02-4, name is Methyl 2-bromo-1-methyl-1H-imidazole-5-carboxylate, molecular formula is C6H7BrN2O2, 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.
Step 1. To a mixture of the Ex 3 hydrochloride (100 mg, 0.243 mol), 2-bromo-3-methyl-3H-imidazole-4- carboxylic acid methyl ester (56 mg, 0.243 mmol), DIPEA (83 uL, 0.486 mmol), 18-crown-6 (1.29 g, 4.86 mmol) and CsF (38 mg, 0.243 mmol) is heated to 120C overnight. The mixture is then evaporated and the residue is purified by prep. HPLC (Prep-HPLC-3 conditions) to give methyl 2-(3-((2-(difluoromethoxy)-6-methylpyridin-3- yl)carbamoyl)-3-(2-isopropylphenyl)azetidin-1 -yl)-1 -methyl-1 H-imidazole-5-carboxylate Ex 18-35 (20 mg, 16%) as a yellow oil. LCMS-1 : tR = 1.16 min, [M+1]+ 514.19.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Methyl 2-bromo-1-methyl-1H-imidazole-5-carboxylate, its application will become more common.
Reference:
Patent; IDORSIA PHARMACEUTICALS LTD; BOLLI, Martin; BROTSCHI, Christine; LESCOP, Cyrille; WILLIAMS, Jodi T.; (0 pag.)WO2019/234115; (2019); A1;,
Imidazole – Wikipedia,
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