Application of 2854-16-2, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.2854-16-2, name is 1-Amino-2-methylpropan-2-ol, molecular formula is C4H11NO, molecular weight is 89.14, as common compound, the synthetic route is as follows.
5-Chloro-3-(4,4-difluorocyclohexylmethyl)-2-trifluor omethylimidazo[1,2-a]pyridine-7-carboxylic acid (28 mg, 0.093 mmol) obtained in step 3 of Example 61 was dissolved in N,N-dimethylformamide (2.0 mL), and the solution was stirred overnight at room temperature after adding EDC·HCl (36 mg, 0.187 mmol), HOBt·H2O (29 mg, 0.187 mmol), and 1-amino-2-methylpropan-2-ol (17 mg, 0.187 mmol). The mixture was extracted with ethyl acetate after adding a sodium hydrogen carbonate aqueous solution. The organic layer was washed with water and saturated brine, and dried over anhydrous sodium sulfate. The solvent was then evaporated under reduced pressure. The residue was purified by preparative thin-layer chromatography (chloroform/methanol=9/1) to give compound 182 (40.4 mg, 85percent). 1H NMR (400 MHz, CDCl3, delta): 7.95 (s, 1H), 7.46 (s, 1H), 6.60 (br s, 1H), 3.49 (d, J = 5.9 Hz, 2H), 3.35 (d, J = 6.9 Hz, 2H), 1.97-1.56 (m, 9H), 1.31 (s, 6H); ESIMS m/z: [M + H]+ 468
The chemical industry reduces the impact on the environment during synthesis 2854-16-2, I believe this compound will play a more active role in future production and life.
Reference:
Patent; Kyowa Hakko Kirin Co., Ltd.; SAWADA, Takashi; DANJO, Tomohiro; MOTOSAWA, Keiichi; FURUTA, Takayuki; ICHIOKA, Maki; SUGAWARA, Masamori; UESAKA, Noriaki; EP2671582; (2013); A1;,
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