تفاعل #9989

ord-c44e3068064646e1832ac5b3443cc9f4

معادلة التفاعل

COC(=O)[C@@H]1CC(C)CN1
(2S)-4-Methylproline methyl ester
O=C([O-])O.[Na+]
sodium hydrogencarbonate
O=C(Cl)OCc1ccccc1
benzyl chloroformate
COC(=O)[C@@H]1CC(C)CN1C(=O)OCc1ccccc1
(2S)-1-benzyloxycarbonyl-4-methylproline methyl ester
المردود 99.0%

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    استخلاصThe reaction mixture was extracted with ethyl acetate
  2. 2
    غسيلThe organic layer was washed with water
  3. 3
    أخرىthe solvent was removed by distillation under reduced pressure

الإجراء التجريبي

(2S)-4-Methylproline methyl ester (0.93 g (6.5 mmol), prepared as described in 2)) was dissolved in toluene (20 ml). To the solution were added an aqueous solution (20 ml) of sodium hydrogencarbonate (1.89 g, 22.5 mmol) and benzyl chloroformate (1.54 ml, 10.8 mmol), and the resulting mixture was stirred at room temperature overnight. The reaction mixture was extracted with ethyl acetate. The organic layer was washed with water and the solvent was removed by distillation under reduced pressure, to give (2S)-1-benzyloxycarbonyl-4-methylproline methyl ester (1.78 g) as a pale yellow oil (yield 99%). All of the compound obtained above was dissolved in tetrahydrofuran (30 ml). To the resulting solution was added lithium borohydride (0.28 g, 13 mmol) in three portions, and the resulting mixture was stirred at room temperature. Ice was added to the mixture and the mixture was stirred for 1 hour. The reaction mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate and the solvent was removed by distillation under reduced pressure. The residue was purified by column chromatography through silica gel (eluent, ethyl acetate:hexane=2:5), to give the title compound (1.07 g) as a pale yellow oil (yield 66%).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07091352B2uspto-grants-2006_08