Analyzing the synthesis route of C9H8N2O2

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-(1H-Benzo[d]imidazol-2-yl)acetic acid, and friends who are interested can also refer to it.

Reference of 13570-08-6, 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. 13570-08-6 name is 2-(1H-Benzo[d]imidazol-2-yl)acetic acid, 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 a stirred solution of compound 80 (tosyiate) (536 mg, 1.36 mmol), compound 79 (200 mg, 1. 13 mmol) and HOBt (230 mg, 1.70 mmol) in 5 mL DCM, was added DIPEA (0.99 mL, 5.7 mmol) drop-wise and stirred at 0 C for 10 min under inert atmosphere. Then EDC-HC1 (283 mg, 1.48 mmol) was added to the reaction mixture and allowed to stir at room temperature for 16 h. After completion [confirmed by TLC (70% EtOAc-Hexane, Rf-0.4) and LC-MS] reaction mixture was partitioned between water (70 mL) and DCM (3×60 mL). Organic layer was separated, dried (MgSCfi) and concentrated. Resultant crude was purified by column chromatography (eluent: 30-65% EtOAc-hexane, S1O2) to yield compound 81 (210 mg, 48.8%) as white solid. Mass [ESI]: m/z. 379.45 [M++l]

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-(1H-Benzo[d]imidazol-2-yl)acetic acid, and friends who are interested can also refer to it.

Reference:
Patent; CYTOSITE BIOPHARMA INC.; BILCER, Geoffrey, Malcolm; KELLY, Terence, Alfred; (190 pag.)WO2019/160916; (2019); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem