(1S,2R)-2-氨基-1-茚满醇

反应条件: temp:110.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2,2,2-trichloroethyl 5-tert-butyl-3-(2-cyanopropan-2-yl)-2-methoxyphenylcarbamate (0.086 g, 0.203 mmol) and (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (0.067 g, 0.223 mmol) in acetonitrile (0.8 mL), N,N-diisopropylethylamine (0.058 mL, 0.333 mmol) was added, the mixture was stirred overnight at 110° C. The reaction mixture was evaporated under reduced pressure and the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40) to obtain 0.044 g of the captioned compound (51% yield). The reaction mixture was evaporated under reduced pressure the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40)

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

实验步骤: A suspension of 2,2,2-trichloroethyl 5-tert-butyl-3-(hydroxymethyl)-2-methoxyphenylcarbamate (1.50 g, 3.90 mmol), (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (1.28 g, 4.29 mmol) and N,N-diisopropylethylamine (2.37 mL, 13.6 mmol) in acetonitrile (19.5 mL) was heated to reflux. After 17 hours, the mixture was allowed to cool and the reaction solution was concentrated under reduced pressure. The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100) to obtain 1.09 g of the captioned compound (73% yield). to cool the reaction solution was concentrated under reduced pressure The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100)

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

实验步骤: A suspension of 2,2,2-trichloroethyl 5-tert-butyl-3-(hydroxymethyl)-2-methoxyphenylcarbamate (1.50 g, 3.90 mmol), (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (1.28 g, 4.29 mmol) and N,N-diisopropylethylamine (2.37 mL, 13.6 mmol) in acetonitrile (19.5 mL) was heated to reflux. After 17 hours, the mixture was allowed to cool and the reaction solution was concentrated under reduced pressure. The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100) to obtain 1.09 g of the captioned compound (73% yield). to cool the reaction solution was concentrated under reduced pressure The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100)

反应条件: temp:110.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2,2,2-trichloroethyl 5-tert-butyl-3-(2-cyanopropan-2-yl)-2-methoxyphenylcarbamate (0.086 g, 0.203 mmol) and (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (0.067 g, 0.223 mmol) in acetonitrile (0.8 mL), N,N-diisopropylethylamine (0.058 mL, 0.333 mmol) was added, the mixture was stirred overnight at 110° C. The reaction mixture was evaporated under reduced pressure and the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40) to obtain 0.044 g of the captioned compound (51% yield). The reaction mixture was evaporated under reduced pressure the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40)

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

实验步骤: A suspension of 2,2,2-trichloroethyl 5-tert-butyl-3-(hydroxymethyl)-2-methoxyphenylcarbamate (1.50 g, 3.90 mmol), (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (1.28 g, 4.29 mmol) and N,N-diisopropylethylamine (2.37 mL, 13.6 mmol) in acetonitrile (19.5 mL) was heated to reflux. After 17 hours, the mixture was allowed to cool and the reaction solution was concentrated under reduced pressure. The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100) to obtain 1.09 g of the captioned compound (73% yield). to cool the reaction solution was concentrated under reduced pressure The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100)

反应条件: temp:110.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2,2,2-trichloroethyl 5-tert-butyl-3-(2-cyanopropan-2-yl)-2-methoxyphenylcarbamate (0.086 g, 0.203 mmol) and (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (0.067 g, 0.223 mmol) in acetonitrile (0.8 mL), N,N-diisopropylethylamine (0.058 mL, 0.333 mmol) was added, the mixture was stirred overnight at 110° C. The reaction mixture was evaporated under reduced pressure and the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40) to obtain 0.044 g of the captioned compound (51% yield). The reaction mixture was evaporated under reduced pressure the obtained residue was purified by silica gel column chromatography (ethyl acetate/n-hexane=10/90-60/40)

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

实验步骤: A suspension of 2,2,2-trichloroethyl 5-tert-butyl-3-(hydroxymethyl)-2-methoxyphenylcarbamate (1.50 g, 3.90 mmol), (1S,2R)-2-amino-2,3-dihydro-1H-indene-1-ol.L-tartaric acid salt (1.28 g, 4.29 mmol) and N,N-diisopropylethylamine (2.37 mL, 13.6 mmol) in acetonitrile (19.5 mL) was heated to reflux. After 17 hours, the mixture was allowed to cool and the reaction solution was concentrated under reduced pressure. The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100) to obtain 1.09 g of the captioned compound (73% yield). to cool the reaction solution was concentrated under reduced pressure The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=50/50-0/100)