Category: 90871-47-9

Reference of 90871-47-9, A common heterocyclic compound, 90871-47-9, name is 2-Amino-1-isopropylbenzimidazole, molecular formula is C10H13N3, 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.

200 mg (0.64 mmol) of compound 2-[(2,5-dichloropyridin-4-yl)amino]-N-methoxybenzamide, 168 mg (0.96 mmol) was added to a 20 ml microwave tube.1-isopropyl-1H-benzo[d]imidazol-2-amine, 417 mg (1.28 mmol) cesium carbonate, 93 mg (0.16 mol) XantPhos, 117 mg (0.128 mmol) Pd2 (dba) 3 and 10 ml of 1,4 – Dioxane, under nitrogen protection, use the oil pump to remove the air in the system, replace it with nitrogen, repeat three times, seal the microwave tube, at 150 C microThe reaction was carried out in a wave reactor for 50 min.After the TLC detection reaction was completed, the catalyst was filtered off with celite, eluted with ethyl acetate, and the solvent was evaporated to dryness, and silica gel column chromatography (gradient elution polarity: PE: EA=100:1 to EA) to collect the crude product 109 mg , the yield is 37.7%,

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; Guangzhou Anyanren Pharmaceutical Technology Co., Ltd.; Xie Dexun; Li Quanwei; Xue Weicai; Liu Hui; (27 pag.)CN108912095; (2018); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 90871-47-9, name is 2-Amino-1-isopropylbenzimidazole, A new synthetic method of this compound is introduced below., Recommanded Product: 2-Amino-1-isopropylbenzimidazole

General procedure: Sodium (0.29 g, 12.5 mmol) was dissolved in 15 mL of anhydrous ethanol and this solution was concentrated to a small volume (2-3 mL), then 5.0 mmol of the proper 1-substituted 1H-benzimidazol-2-amine 8 and 50.0 mmol (8.00 g) of diethyl malonate were added and the resulting mixture was heated at 150 C (under reflux) with stirring for 3 h. After cooling, the sodium salt of compound 9, which precipitated as a whitish solid during the reaction, was collected, crushed in a mortar, suspended in Et2O, filtered and dried. This solid was then dissolved in water and the resulting solution was acidified with an excess of 6 N aq HCl (or carefully acidified with 6 N aq HCl down to pH 4, in the case of the pyridyl derivatives compounds 9h-k): this way compounds 9a-k separated out as white or whitish solids that were collected by filtration, washed with water, dried and crystallized from the proper solvent. Only in the case of compounds 9l-o (bearing a tertiary amino group on the side chain), the aqueous solution of sodium salt was treated with an excess of 70% aq. HClO4 to get the precipitation of compounds 9l-o as water-insoluble perchlorates which were collected by filtration, washed with water, dried and crystallized from ethanol. According to this procedure the following compounds 9 were obtained (IR and 1H NMR data are reported only for the new compounds).

The synthetic route of 90871-47-9 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Di Braccio, Mario; Grossi, Giancarlo; Signorello, Maria Grazia; Leoncini, Giuliana; Cichero, Elena; Fossa, Paola; Alfei, Silvana; Damonte, Gianluca; European Journal of Medicinal Chemistry; vol. 62; (2013); p. 564 – 578;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem