4-fluoro-2-methoxybenzoyl chloride

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: By using 5-(4-aminophenyl)-1H-naphtho[1,2-b][1,4]diazepine-2,4(3H,5H)-dione obtained in Example 1, (3), and 4-fluoro-2-methoxybenzoyl chloride, the title compound (yield 62%) was obtained in the same manner as that of Example 1, (4).

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: By using 5-(4-aminophenyl)-1H-naphtho[1,2-b][1,4]diazepine-2,4(3H,5H)-dione obtained in Example 1, (3), and 4-fluoro-2-methoxybenzoyl chloride, the title compound (yield 62%) was obtained in the same manner as that of Example 1, (4).

反応条件: temp:0.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To 231 parts of a aziridine solution 0.95M in water are added 16 parts of sodium hydrogen carbonate while stirring vigorously at 0° C. Then there is added dropwise, during a 45 minutes-period, a solution of 36 parts of 4-fluoro-2-methoxybenzoyl chloride in 150 parts of trichloromethane while still cooling at 0° C. Upon completion, stirring is continued for 30-45 minutes without cooling. The reaction mixture is adjusted to pH 8 with a diluted sodium hydroxide solution and the product is extracted three times with trichloromethane. The combined extracts are washed three times with water, dried, filtered and evaporated, yielding 40.5 parts of 1-(4-fluoro-2-methoxybenzoyl)-aziridine as a residue. Then there is added dropwise, during a 45 minutes-period Upon completion, stirring without cooling the product is extracted three times with trichloromethane The combined extracts are washed three times with water dried filtered evaporated

反応条件: temp:0.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To 231 parts of a aziridine solution 0.95M in water are added 16 parts of sodium hydrogen carbonate while stirring vigorously at 0° C. Then there is added dropwise, during a 45 minutes-period, a solution of 36 parts of 4-fluoro-2-methoxybenzoyl chloride in 150 parts of trichloromethane while still cooling at 0° C. Upon completion, stirring is continued for 30-45 minutes without cooling. The reaction mixture is adjusted to pH 8 with a diluted sodium hydroxide solution and the product is extracted three times with trichloromethane. The combined extracts are washed three times with water, dried, filtered and evaporated, yielding 40.5 parts of 1-(4-fluoro-2-methoxybenzoyl)-aziridine as a residue. Then there is added dropwise, during a 45 minutes-period Upon completion, stirring without cooling the product is extracted three times with trichloromethane The combined extracts are washed three times with water dried filtered evaporated

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was prepared using methods analogous to those described in Synthesis 1-A, 1-B, 1-D and 2, replacing 2-methoxybenzoyl chloride with 2-methoxy-4-fluorobenzoyl chloride in Synthesis 1A, and replacing (R)-3-aminopiperidine-1-carboxylic acid tert-butyl ester with trans-1-tert-butyl 3-ethyl 4-(2-(5-fluoro-2-hydroxyphenyl)-3,4-dihydroquinazolin-4-ylamino)pyrrolidine-1,3-dicarboxylate in Synthesis 2-A.

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: By using 5-(4-aminophenyl)-1H-naphtho[1,2-b][1,4]diazepine-2,4(3H,5H)-dione obtained in Example 1, (3), and 4-fluoro-2-methoxybenzoyl chloride, the title compound (yield 62%) was obtained in the same manner as that of Example 1, (4).

反応条件: temp:0.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To 231 parts of a aziridine solution 0.95M in water are added 16 parts of sodium hydrogen carbonate while stirring vigorously at 0° C. Then there is added dropwise, during a 45 minutes-period, a solution of 36 parts of 4-fluoro-2-methoxybenzoyl chloride in 150 parts of trichloromethane while still cooling at 0° C. Upon completion, stirring is continued for 30-45 minutes without cooling. The reaction mixture is adjusted to pH 8 with a diluted sodium hydroxide solution and the product is extracted three times with trichloromethane. The combined extracts are washed three times with water, dried, filtered and evaporated, yielding 40.5 parts of 1-(4-fluoro-2-methoxybenzoyl)-aziridine as a residue. Then there is added dropwise, during a 45 minutes-period Upon completion, stirring without cooling the product is extracted three times with trichloromethane The combined extracts are washed three times with water dried filtered evaporated