tert-butyl 3-amino-3-cyclopropylbutanoate

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

实验步骤: The title compound was synthesized in analogy to Example 112e, using 5-Cyclopropyl-4-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid (example 68a) and tert-butyl 3-amino-3-cyclopropyl-butanoate (example 229b) as starting materials and isolated (467 mg, 56%); MS (ESI, m/z): 457.6 (M+H+). isolated (467 mg, 56%)

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

实验步骤: The title compound was synthesized in analogy to Example 112e, using 5-Cyclopropyl-4-(2,2,2-trifluoro-ethoxy)-pyridine-2-carboxylic acid (Example 48c) and tert-butyl 3-amino-3-cyclopropyl-butanoate (example 229b) as starting materials and isolated (890 mg, 88%); MS (ESI, m/z): 443.6 (M+H+). isolated (890 mg, 88%)

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

实验步骤: tert-butyl 3-(tert-butylsulfinylamino)-3-cyclopropyl-butanoate (example 229a, 1.93 g, 6.36 mmol) was dissolved in a 4M solution of hydrochloric acid in dioxane (4.77 ml, 19.1 mmol) and the reaction mixture was stirred at room temperature for 30 minutes. The reaction was then diluted with ethyl acetate and poured into a separatory funnel. The organic phase was extracted with a 2M aqueous solution of sodium carbonate. The organic phase was dried over sodium sulfate and evaporated down to dryness to yield the title compound (1.08 g, 85%) as a crude oil which was used without any purification. MS (ESI, m/z): 200.3 (M+H+). poured into a separatory funnel The organic phase was extracted with a 2M aqueous solution of sodium carbonate The organic phase was dried over sodium sulfate evaporated down to dryness