3-piperazin-1-ylpropane-1,2-diol

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Grams 6.4 of 1-(2,3-dihydroxypropyl)piperazine and 3.3 g of 2-bromo-1,3-thiazole in 50 ml dioxane were refluxed for 24 hours. The reaction mixture was evaporated to dryness and the so obtained residue was purified on column eluting with chloroform:methanol (9:1). Grams 1.5 of 3-[4-(1,3-thiazol-2-yl)piperazin-1-yl] propane-1,2-diol which, by recrystallization from acetone, melted at 138°-139° C., were obtained. The reaction mixture was evaporated to dryness the so obtained residue was purified on column eluting with chloroform:methanol (9:1) Grams 1.5 of 3-[4-(1,3-thiazol-2-yl)piperazin-1-yl] propane-1,2-diol which, by recrystallization from acetone, melted at 138°-139° C. were obtained

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Grams 20.5 of 1-(2,3-dihydroxypropyl)piperazine and 11 g of 3-chloropyrazine-2-carboxylic acid methyl ester in 100 ml dioxane were refluxed for one hour. The reaction mixture was cooled and settled, the solvent evaporated and the obtained residue dissolved in concentrated hydrochloric acid and the solution diluted with isopropanol until incipient precipitation. After resting, 12.7 g of 3-[4-(2,3-dihydroxypropyl)piperazin-1-yl]pyrazine-2-carboxylic acid methyl ester dihydrochloride melting at 195°-197° C. (with decomposition), were obtained. The reaction mixture was cooled the solvent evaporated the obtained residue dissolved in concentrated hydrochloric acid the solution diluted with isopropanol until incipient precipitation

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Grams 4.6 of 2-methylthio-4-chloropyrimidine-5-carboxylic acid ethyl ester and 6.4 g of 1-(2,3-dihydroxypropyl)piperazine in 50 ml dioxane were refluxed for 30 minutes. The mixture was cooled and settled, then the solvent was evaporated and the dried residue purified on column eluting with chloroform:methanol (9:1). Grams 4.8 of 2-methylthio-4-[4-(2,3-dihydroxypropyl)piperazin-1-yl]pyrimidine-5-carboxylic acid ethyl ester as an oil, were obtained. The mixture was cooled the solvent was evaporated the dried residue purified on column eluting with chloroform:methanol (9:1)