(E)-2-(4-chlorophenyl)ethenesulfonyl chloride

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

実験手順: In the same manner as in Referential Example 1, a reaction was conducted using tert-butyl 1-piperazinecarboxylate and (E)-4-chlorostyrylsulfonyl chloride as starting materials, whereby the title compound was obtained.

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

実験手順: In a similar manner to Referential Example 1 except for the use of tert-butyl 1-piperazinecarboxylate and (E)-4-chlorostyrylsulfonyl chloride as the raw materials, the reaction was conducted, whereby the title compound was obtained.

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

実験手順: A solution of (E)-4-chlorostyrylsulfonyl chloride (10 mmol) and 2-chloroaniline (10 mmol) was subjected to General Procedure 1, part B. The title compound, melting point 107-109° C., was obtained in 57.8% yield.

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

実験手順: A solution of (E)-4-chlorostyrylsulfonyl chloride (10 mmol) and 3-chloroaniline (10 mmol) was subjected to General Procedure 1, part B. The title compound, melting point 118-120° C., was obtained in 31.8% yield.

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

実験手順: A solution of (E)-4-chlorostyrylsulfonyl chloride (10 mmol) and 4-fluoroaniline (10 mmol) was subjected to General Procedure 1, part B. The title compound, melting point 105-107° C., was obtained in 68.5% yield.

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

実験手順: In the same manner as in Referential Example 1, a reaction was conducted using tert-butyl 1-piperazinecarboxylate and (E)-4-chlorostyrylsulfonyl chloride as starting materials, whereby the title compound was obtained.

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

実験手順: Using an analogous procedure to that described in Example 2, 2-amino-N-{1-piperidinocarbonyl-2-[1-(4-pyridyl)piperidin-4-ylcarbonylamino]ethyl}acetamide hydrochloride salt was reacted with (E)-4-chlorostyrylsulphonyl chloride to give 2-[(E)-4-chlorostyrylsulphonamido]-N -[1-piperidinocarbonyl-2-{1-(4-pyridyl)piperidin-4-ylcarbonylamino]ethyl}acetamide as a gum (0.1 g, 16%);

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

実験手順: The title compound was synthesized as described for 226 a) in 61% yield, starting from 2-amino-5-chloro-4-fluorobenzenesulfonamide and (E)-2-(4-chlorophenyl)ethenesulfonyl chloride.

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

実験手順: Using an analogous procedure to that described in Example 2, 2-amino-N-{1-piperidinocarbonyl-2-[1-(4-pyridyl)piperidin-4-ylcarbonylamino]ethyl}acetamide hydrochloride salt was reacted with (E)-4-chlorostyrylsulphonyl chloride to give 2-[(E)-4-chlorostyrylsulphonamido]-N-{1-piperidinocarbonyl-2-[1-(4-pyridyl)piperidin-4-ylcarbonylamino]-ethyl}acetamide as a gum (0.1 g, 16%);

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

実験手順: Using an analogous procedure to that described in Example 2, 2-amino-N-{1-piperidinocarbonyl-2-[1-(4-pyridyl)piperidin-4-ylcarbonylamino]ethyl}acetamide hydrochloride salt was reacted with (E)-4-chlorostyrylsulphonyl chloride to give 2-[(E)-4-chlorostyrylsulphonamido]-N-{1-piperidinocarbonyl-2-[1-(4-pyridyl)piperidin-4-ylcarbonylamino]-ethyl}acetamide as a gum (0.1 g, 16%);

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

実験手順: In a similar manner to Referential Example 1 except for the use of tert-butyl 1-piperazinecarboxylate and (E)-4-chlorostyrylsulfonyl chloride as the raw materials, the reaction was conducted, whereby the title compound was obtained.

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

実験手順: A solution of (E)-4-chlorostyrylsulfonyl chloride (10 mmol) and 2-chloroaniline (10 mmol) was subjected to General Procedure 1, part B. The title compound, melting point 107-109° C., was obtained in 57.8% yield.