(S)-1-N-Boc-2-乙基哌嗪

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

实验步骤: A solution of the product from example 69 part c) (6.09 g) and 10% Pd/C (1.14 g) in EtOH (85 mL) was hydrogenated at 3.8 bar for 16 h. The reaction mixture was filtered through Celite and the filtrate concentrated in vacuo to give the sub-title compound as an oil (3.65 g). The reaction mixture was filtered through Celite the filtrate concentrated in vacuo

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

实验步骤: Beginning with 1.45 gm (5.47 mMol) 4-trifluoromethyl-7-bromobenzofuran and 1.4 gm (6.53 mMol) 1-(tert-butoxycarbonyl)-2(S)-ethylpiperazine, 1.82 gm (84%) of the desired compound were prepared essentially as described in Example 1.

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

实验步骤: The title compound was prepared as a solid according to the method of Example 81 using the product of Example 75 step i) and (S)-2-ethyl-piperazine-1-carboxylic acid, tert-butyl ester.

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

实验步骤: The title compound was prepared as a solid according to the method of Example 81 using the product of Example 75 step i) and (S)-2-ethyl-piperazine-1-carboxylic acid, tert-butyl ester.

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

实验步骤: A solution of the product from example 69 part c) (6.09 g) and 10% Pd/C (1.14 g) in EtOH (85 mL) was hydrogenated at 3.8 bar for 16 h. The reaction mixture was filtered through Celite and the filtrate concentrated in vacuo to give the sub-title compound as an oil (3.65 g). The reaction mixture was filtered through Celite the filtrate concentrated in vacuo

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

实验步骤: A solution of the product from example 69 part c) (6.09 g) and 10% Pd/C (1.14 g) in EtOH (85 mL) was hydrogenated at 3.8 bar for 16 h. The reaction mixture was filtered through Celite and the filtrate concentrated in vacuo to give the sub-title compound as an oil (3.65 g). The reaction mixture was filtered through Celite the filtrate concentrated in vacuo

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

实验步骤: Heat a mixture of 1-chloro-4-(4-fluorophenyl)phthalazine (5.02 g, 19.4 mmol), (S)-tert-butyl 2-ethylpiperazine-1-carboxylate (5.00 g, 23.3 mmol) and K2CO3 (5.38 g, 38.9 mmol) in DMSO (75 mL) at 120° C. for 1 d. Pour the reaction mixture into water, rinsing with EtOAc. Extract with EtOAc. Wash the organic layer with water (2×), then brine, dry over Na2SO4, and concentrate under reduced pressure. Purify the resulting residue by flash silica gel chromatography (gradient of 20 to 80% EtOAc in hexanes) to provide the title compound (5.11 g, 60%). ES/MS m/z 437.2 (M+1). Heat rinsing with EtOAc Extract with EtOAc Wash the organic layer with water (2×) brine, dry over Na2SO4 concentrate under reduced pressure Purify the resulting residue by flash silica gel chromatography (gradient of 20 to 80% EtOAc in hexanes)

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

实验步骤: Beginning with 1.45 gm (5.47 mMol) 4-trifluoromethyl-7-bromobenzofuran and 1.4 gm (6.53 mMol) 1-(tert-butoxycarbonyl)-2(S)-ethylpiperazine, 1.82 gm (84%) of the desired compound were prepared essentially as described in Example 1.

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

实验步骤: The title compound was prepared as a solid according to the method of Example 81 using the product of Example 75 step i) and (S)-2-ethyl-piperazine-1-carboxylic acid, tert-butyl ester.