2,2-二甲基氮丙啶

反应条件: temp:0.00; pressure:0.00; stir:

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethyamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethyamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethylamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethylamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 234 g of 2-mercaptoethanol are dissolved in 90 ml of dimethoxyethane. 63.3 g of 2,2-dimethylaziridine are added dropwise to this solution and the mixture is stirred at 70° C. for 4 hours and concentrated, and the residue is distilled in a water jet vacuum. B.p.: 141°-142° C. (at 20 mbar); M.p.: 49°-51°; concentrated the residue is distilled in a water jet vacuum

反应条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 234 g of 2-mercaptoethanol are dissolved in 90 ml of dimethoxyethane. 63.3 g of 2,2-dimethylaziridine are added dropwise to this solution and the mixture is stirred at 70° C. for 4 hours and concentrated, and the residue is distilled in a water jet vacuum. B.p.: 141°-142° C. (at 20 mbar); M.p.: 49°-51°; concentrated the residue is distilled in a water jet vacuum

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethylamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 2,2-Dimethyl aziridine is dissolved in CH2Cl2 and triethylamine under argon at 0° C. Benzylchloroformate is added and the contents of the flask are stirred at room temperature overnight. The mixture is poured into 10% citric acid and extracted with CHCl3. The organic layer is washed with dilute aqueous NaHCO3 and dried over MgSO4. The solution is evaporated to yield N-Cbz-2,2-dimethylaziridine. at 0° C extracted with CHCl3 The organic layer is washed with dilute aqueous NaHCO3 dried over MgSO4 The solution is evaporated

反应条件: temp:0.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2,2-dimethylaziridine (5.42 g; 0.076 mole; sold by Polysciences, Inc., Warrington, PA) in pyridine (100 mL) cooled in an ice bath, is added p-toluenesulfonyl chloride (21.81 g; 0.114 mole) in one portion. The reaction is stirred at 0° C. for 2 hours; diluted with ether (400 mL); washed with cold 10% H3PO4 (2×150 mL), with a saturated NaHCO3 solution (3×150 mL) and brine (1×150 mL); and dried over MgSO4. Rotary evaporation of the solution affords a yellowish solid which is crystallized from ethyl acetate to yield the product 2,2-dimethyl-N-p-toluenesulfonyl-aziridine (4.48 g). 1H NMR (CDCl3):1.53 (6H, s), 2.45 (5H, m), 7.2-8.0 ppm (4H, m, aromatics). washed with cold 10% H3PO4 (2×150 mL), with a saturated NaHCO3 solution (3×150 mL) and brine (1×150 mL) and dried over MgSO4 Rotary evaporation of the solution affords a yellowish solid which is crystallized from ethyl acetate

反应条件: temp:-40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 0.08 moles of triethylamine, 0.025 moles of POCl3 and 150 milliliters of dried tetrahydrofuran were combined in a 250 milliliter round bottom flask, under a nitrogen atmosphere to avoid moisture contamination, to form a first solution which was then cooled to -40° C. A second solution was then prepared containing 0.05 moles of 2,2-dimethylaziridine in 20 milliliters of THF and the second solution was added dropwise to the cooled first solution over a period of about 2 hours. The resulting slurry was then warmed over a period of about 1 hour to 0° C. then cooled again to -30° C. and then had added thereto, by dropwise addition, a solution containing 0.026 moles of 3-methoxypropyl amine in 20 milliliters of THF. The solution was then allowed to stand overnight with constant stirring at ambient temperature, the resulting slurry was filtered, the filtrate was concentrated by rotary evaporation, and thereafter vacuum distilled at 130° C./0.42 millimeters Hg to produce a 60% yield of 3-methoxypropylamino phosphoraziridine. NMR characterization indicated that the product was 95% pure. to form a first solution which A second solution was then prepared the second solution was added dropwise to the cooled first solution over a period of about 2 hours The resulting slurry was then warmed over a period of about 1 hour to 0° C. then cooled again to -30° C. had added by dropwise addition the resulting slurry was filtered the filtrate was concentrated by rotary evaporation vacuum distilled at 130° C./0.42 millimeters Hg

反应条件: temp:-40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 0.08 moles of triethylamine, 0.025 moles of POCl3 and 150 milliliters of dried tetrahydrofuran were combined in a 250 milliliter round bottom flask, under a nitrogen atmosphere to avoid moisture contamination, to form a first solution which was then cooled to -40° C. A second solution was then prepared containing 0.05 moles of 2,2-dimethylaziridine in 20 milliliters of THF and the second solution was added dropwise to the cooled first solution over a period of about 2 hours. The resulting slurry was then warmed over a period of about 1 hour to 0° C. then cooled again to -30° C. and then had added thereto, by dropwise addition, a solution containing 0.026 moles of 3-methoxypropyl amine in 20 milliliters of THF. The solution was then allowed to stand overnight with constant stirring at ambient temperature, the resulting slurry was filtered, the filtrate was concentrated by rotary evaporation, and thereafter vacuum distilled at 130° C./0.42 millimeters Hg to produce a 60% yield of 3-methoxypropylamino phosphoraziridine. NMR characterization indicated that the product was 95% pure. to form a first solution which A second solution was then prepared the second solution was added dropwise to the cooled first solution over a period of about 2 hours The resulting slurry was then warmed over a period of about 1 hour to 0° C. then cooled again to -30° C. had added by dropwise addition the resulting slurry was filtered the filtrate was concentrated by rotary evaporation vacuum distilled at 130° C./0.42 millimeters Hg