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Intermediate 2a (2Og) is dissolved in DMF (15OmL) and carbonyldiimidazole (19g) is added. The reaction is then heated to 70C for 1 hour after which the reaction is cooled to room temperature. Aminoacetaldehyde diethylacetal (16.5mL) is added and allowed to react at room temperature overnight. The solvent is then removed under reduced pressure and the residue is purified by LC (SiO2, DCM:MeOH 90: 10) to yield the desired compound 1 (1 Og).
The chemical industry reduces the impact on the environment during synthesis 2-Oxoindoline-6-carboxylic acid. I believe this compound will play a more active role in future production and life.
Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG; WO2006/64044; (2006); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem