Downstream synthetic route of 17782-81-9

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.17782-81-9,Imidazo[2,1-b]thiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of the respective carboxylic acid (0.029 mmol, 1.3eq) in DMF (0.20 mL) is added successively a solution of DIPEA (0.08 mmol, 3.5eq) in DMF (0.15 mL) and a solution of TBTU (0.024 mmol, 1.05eq) in DMF (0.15 mL). The obtained mixture is treated with a solution of the respective 2-aza-bicyclo[3.1.0]hexane derivative (0.023 mmol, l.Oeq) in DMF (0.40 mL). The mixture is shaken over night and purified by prep. HPLC to give the respective amide derivatives. Example 35 imidazo[2,l-b]thiazole-5-carboxylic acid {(lS,3S,5S)-2-[5-(3-fluoro-phenyl)-2-methyl- thiazole-4-carbonyl]-2-aza-bicyclo[3.1.0]hex-3-ylmethyl}-amide prepared by reaction of [(lS,3S,5S)-3-aminomethyl-2-aza-bicyclo[3.1.0]hex-2-yl]-[5-(3- fluoro-phenyl)-2-methyl-thiazol-4-yl]-methanone with imidazo[2,l-b]thiazole-5- carboxylic acid. LC-MS (basic): tR = 0.80 min; [M+H]+ = 482.1., 17782-81-9

The synthetic route of 17782-81-9 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ACTELION PHARMACEUTICALS LTD; WO2008/81399; (2008); A2;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica