Electric Literature of 51454-63-8, 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.51454-63-8, name is 2-(Hydroxymethyl)isonicotinonitrile, molecular formula is C7H6N2O, molecular weight is 134.14, as common compound, the synthetic route is as follows.
To a cooled solution of oxalyl chloride (13.2mL, 150mmol) in anhydrous DCM (86mL) under nitrogen atmosphere at -78C was added DMSO (21.2ml_ dropwise over 20 minutes. The mixture was stirred for 15 minutes at (-78C) before 2-hydroxymethyl-isonicotinonitrile (4.0g, 30 mmol) dissolved in anhydrous DCM (60mL) was added dropwise to the reaction mixture over 5 minutes. The reaction was stirred for 2 hrs at -78C maintaining a nitrogen atmosphere. A white solid precipitate formed and the temperature was raised to (-55C) and triethylamine (6.15mL, 450mmol) was added dropwise for over 15 minutes, cooling bath was removed allowing the mixture to warm to room temperature over 2 hrs. The mixture was diluted with DCM (400ml_) and washed with brine (2x 50mL). The aqueous phase was extracted with DCM (3x 50 ml_). The combined organic layers were combined and concentrated in vacuo. A buff white solid was isolated that was used without any further purification. Single peak in LC-MS analysis, (yield taken to be quantitative), m/z (LC-MS, ESP), RT=2.53mins, (M+H)=133.0.
Statistics shows that 51454-63-8 is playing an increasingly important role. we look forward to future research findings about 2-(Hydroxymethyl)isonicotinonitrile.
Reference:
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2006/21801; (2006); A1;,
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