2,3-二氢-1H-吲哚-3-基甲醇

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

实验步骤: 85 mg (0.25 mmol) 6-[4-(2-oxo-2,3-dihydroimidazo[4,5-b]pyridin-1-yl)-piperidin-1-yl]-pyrimidine-4-carboxylic acid and 50 mg (0.32 mmol) (2,3-dihydro-1H-indol-3-yl)-methanol in 50 μL (0.36 mmol) TEA and 0.90 mL DMF were combined with 85 mg (0.27 mmol) TBTU and stirred for 5 h at RT. Then the reaction mixture was purified by preparative HPLC-MS. The product-containing fractions were combined and freeze-dried. Then the reaction mixture was purified by preparative HPLC-MS freeze-dried

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

实验步骤: 100 mg (0.25 mmol) of 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-pyrimidine-4-carboxylic acid and 50 mg (0.32 mmol) (2,3-dihydro-1H-indol-3-yl)-methanol in 50 μL (0.27 mmol) TEA and 0.90 mL DMF were combined with 85 mg (0.27 mmol) TBTU and the mixture was stirred for 5 h at RT. Then the reaction mixture was purified by preparative HPLC-MS. The product-containing fractions were combined and evaporated down by roughly half. The precipitated solid was suction filtered and dried. Then the reaction mixture was purified by preparative HPLC-MS evaporated down by roughly half filtered dried

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

实验步骤: 0.79 g (3.5 mmol) ethyl 2,3-dihydro-1H-indol-3-carboxylate were added batchwise at RT to 7.8 mL (7.8 mmol) of a 1 M lithium aluminium hydride solution (in THF) in 40 mL THF and refluxed for 1 h. Then the reaction mixture was combined with water while being cooled, the precipitate formed was filtered off and the filtrate was evaporated down. refluxed for 1 h while being cooled the precipitate formed was filtered off the filtrate was evaporated down

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

实验步骤: 100 mg (0.24 mmol) 6-(2′-oxo-1,1′,2′,3-tetrahydrospiro[indene-2,3′-pyrrolo[2,3-b]pyridin]-5-ylamino)pyrimidine-4-carboxylic acid hydrochloride, 45 mg (0.30 mmol) (2,3-dihydro-1H-indol-3-yl)-methanol, 0.10 mL (0.71 mmol) TEA and 88 mg (0.27 mmol) TBTU in 1.0 mL DMF were stirred overnight at RT. The purification was carried out by preparative HPLC-MS. The product-containing fractions were combined and the solvent was evaporated down by about half. The precipitate formed was suction filtered and dried. The purification the solvent was evaporated down by about half The precipitate formed filtered dried

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

实验步骤: 0.79 g (3.5 mmol) ethyl 2,3-dihydro-1H-indole-3-carboxylate were added batchwise at RT to 7.8 mL (7.8 mmol) of a 1 molar lithium aluminium hydride-THF solution in 40 mL THF and the mixture was refluxed for 1 h. Then the reaction mixture was decomposed with water, while cooling, the precipitate formed was filtered off and the filtrate was evaporated down. the mixture was refluxed for 1 h while cooling the precipitate formed was filtered off the filtrate was evaporated down