Extracurricular laboratory: Synthetic route of 2-Chloro-7-methyl-1H-benzo[d]imidazole

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-Chloro-7-methyl-1H-benzo[d]imidazole, and friends who are interested can also refer to it.

Related Products of 15965-57-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 15965-57-8 name is 2-Chloro-7-methyl-1H-benzo[d]imidazole, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

To 2-chloro-7-methyl-1H-benzo[d]imidazole (0.65 g, 3.9 mmol) from example 10, step A, in THF (35 mL) was added n-butyllithium (1.6 mL, 3.9 mmol) dropwise at -78C. After 45 minutes, a solution of racemic (1′-azaspiro[oxirane-2,3′-bicyclo[2.2.2]octan]-1′-yl-4-ium)trihydroborate (0.66 g, 4.29 mmol) from the reference example, in THF (10 mL) was added dropwise at -78C. The cooling bath ws removed and the reaction mixture warmed to room temperature. After 15 minutes, the mixture was heated to 75C for 2 hours and then cooled to room temperature. The reaction was quenched with water and the product was extracted with ethyl acetate (100 mL). The organics were dried with MgSO4, filtered and the solvent was removed to yield the crude product. The crude material was purified by chromatography (Biotage) to yield racemic (8-methyl-3H-1′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,3′-bicyclo[2.2.2]octan]-1′-yl-10-ium)trihydroborate (0.40 g, 1.4 mmol, 52%). The 5-methyl regioisomer product was not observed. MS (LC/MS) R.T. = 1.90; [M+1-BH3]+ = 270.07.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-Chloro-7-methyl-1H-benzo[d]imidazole, and friends who are interested can also refer to it.

Reference:
Article; Cook, James; Zusi, F. Christopher; Hill, Matthew D.; Fang, Haiquan; Pearce, Bradley; Park, Hyunsoo; Gallagher, Lizbeth; McDonald, Ivar M.; Bristow, Linda; Macor, John E.; Olson, Richard E.; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5002 – 5005;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The important role of 15965-57-8

The synthetic route of 15965-57-8 has been constantly updated, and we look forward to future research findings.

15965-57-8, name is 2-Chloro-7-methyl-1H-benzo[d]imidazole, belongs to imidazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: 15965-57-8

Step B: (8-Methyl-3H-l ‘-azaspiro[benzo[4,5]imidazo[2, l-b]oxazole-2,3 ‘- bicyclo[2.2.2]octan]-l ‘-yl-8-ium)trihydroborate To 2-chloro-7-methyl-lH-benzo[d]imidazole (0.65 g, 3.9 mmol) from example 10, step A, in THF (35 mL) was added n-butyllithium (1.6 mL, 3.9 mmol) dropwise at – 78C. After 45 minutes, a solution of racemic (l’-azaspiro[oxirane-2,3′- bicyclo[2.2.2]octan]-l’-yl-4-ium)trihydroborate (0.66 g, 4.29 mmol) from the reference example, in THF (10 mL) was added dropwise at -78C. The cooling bath ws removed and the reaction mixture warmed to room temperature. After 15 minutes, the mixture was heated to 75C for 2 hours and then cooled to room temperature. The reaction was quenched with water and the product was extracted with ethyl acetate (100 mL). The organics were dried with MgS04, filtered and the solvent was removed to yield the crude product. The crude material was purified by chromatography (Biotage) to yield racemic (8-methyl-3H-l’-azaspiro[benzo[4,5]imidazo[2, l-b]oxazole-2,3′-bicyclo[2.2.2]octan]-r- yl-10-ium)trihydroborate (0.40 g, 1.4 mmol, 52%). The 5-methyl regioisomer product was not observed. MS (LC/MS) R.T. = 1.90; [M+1-BH3]+ = 270.07.

The synthetic route of 15965-57-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; COOK II, James H.; ZUSI, F. Christopher; HILL, Matthew D.; (87 pag.)WO2016/73407; (2016); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem