Electric Literature of 534-03-2, 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.534-03-2, name is 2-Aminopropane-1,3-diol, molecular formula is C3H9NO2, molecular weight is 91.1091, as common compound, the synthetic route is as follows.
Intermediate 131: 2-(l,3-Dihvdroxypropan-2-yl)isoindoline-l,3-dione (0848) To a stirring solution of 2-aminopropane-l,3-diol (327.2 mg, 3.59 mmol, commercially available from, for example, Sigma-Aldrich) in DMF (15 ml.) was added phthalic anhydride (533.6 mg, 3.60 mmol) portionwise. The resulting colourless solution was stirred at 90 C under nitrogen for 5 h, after which the reaction mixture was cooled to rt and the volatiles evaporated in vacuo. This was partitioned between ethyl acetate (25 ml.) and water (25 ml.) and the layers separated. The aqueous phase was extracted with further ethyl acetate (4 x 25 ml.) and the organic layers combined and filtered through a cartridge fitted with a hydrophobic frit. The filtrate was evaporated in vacuo. This was redissolved in ethyl acetate (approx. 4 ml.) and 3: 1 ethyl acetate :ethanol (approx. 4 ml.) and directly applied to the top of a 25 g SNAP cartridge and purified by flash column chromatography. The column was eluted with a gradient of 0% – 40% (3: 1 ethyl acetate:ethanol) in cyclohexane. The appropriate fractions were combined and evaporated in vacuo to give 2-(l,3-dihydroxypropan-2- yl)isoindoline-l,3-dione (380.0 mg, 1.72 mmol, 48 % yield) as a white solid. (0849) LCMS (2 min High pH): Rt = 0.55 min, [MH]+ = 222.3.
The chemical industry reduces the impact on the environment during synthesis 534-03-2, I believe this compound will play a more active role in future production and life.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED; ATKINSON, Stephen John; DEMONT, Emmanuel Hubert; HARRISON, Lee Andrew; LEVERNIER, Etienne; PRESTON, Alexander G; SEAL, Jonathan Thomas; WALL, Ian David; WATSON, Robert J; WOOLVEN, James Michael; (225 pag.)WO2017/174621; (2017); A1;,
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