tert-butyl N-[2-amino-1-(2-chlorophenyl)ethyl]carbamate

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A solution of 330 mg (1.15 mmol) of the compound from Example 113A in 7 ml of pyridine was admixed at RT with 177 μl (2.29 mmol) of methanesulphonyl chloride. After 1 h the volatile constituents were removed on a rotary evaporator. The residue is purified by preparative HPLC [Method 23]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 312 mg (78% of theory) of the title compound. After 1 h the volatile constituents were removed on a rotary evaporator The residue is purified by preparative HPLC [Method 23] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Of the compound from Example 113A, 330 mg (1.15 mmol) in 12 ml of water/methanol 1:1 were admixed at RT with 279 mg (3.44 mmol) of potassium cyanate. The mixture was heated at 40° C. for 1 h and then admixed with 1.15 ml of 1M hydrochloric acid (1.15 mmol) and stirred overnight at RT. A further 93 mg (1.14 mmol) of potassium cyanate were added and the mixture was stirred further at RT for 3 h. The entire reaction mixture was purified by preparative HPLC [Method 10]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 292 mg (80% of theory) of the title compound. the mixture was stirred further at RT for 3 h The entire reaction mixture was purified by preparative HPLC [Method 10] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A solution of 330 mg (1.15 mmol) of the compound from Example 113A in 7 ml of pyridine was admixed at RT with 177 μl (2.29 mmol) of methanesulphonyl chloride. After 1 h the volatile constituents were removed on a rotary evaporator. The residue is purified by preparative HPLC [Method 23]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 312 mg (78% of theory) of the title compound. After 1 h the volatile constituents were removed on a rotary evaporator The residue is purified by preparative HPLC [Method 23] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Of the compound from Example 113A, 330 mg (1.15 mmol) in 12 ml of water/methanol 1:1 were admixed at RT with 279 mg (3.44 mmol) of potassium cyanate. The mixture was heated at 40° C. for 1 h and then admixed with 1.15 ml of 1M hydrochloric acid (1.15 mmol) and stirred overnight at RT. A further 93 mg (1.14 mmol) of potassium cyanate were added and the mixture was stirred further at RT for 3 h. The entire reaction mixture was purified by preparative HPLC [Method 10]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 292 mg (80% of theory) of the title compound. the mixture was stirred further at RT for 3 h The entire reaction mixture was purified by preparative HPLC [Method 10] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A solution of 330 mg (1.15 mmol) of the compound from Example 113A in 7 ml of pyridine was admixed at RT with 177 μl (2.29 mmol) of methanesulphonyl chloride. After 1 h the volatile constituents were removed on a rotary evaporator. The residue is purified by preparative HPLC [Method 23]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 312 mg (78% of theory) of the title compound. After 1 h the volatile constituents were removed on a rotary evaporator The residue is purified by preparative HPLC [Method 23] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A solution of 330 mg (1.15 mmol) of the compound from Example 113A in 7 ml of pyridine was admixed at RT with 177 μl (2.29 mmol) of methanesulphonyl chloride. After 1 h the volatile constituents were removed on a rotary evaporator. The residue is purified by preparative HPLC [Method 23]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 312 mg (78% of theory) of the title compound. After 1 h the volatile constituents were removed on a rotary evaporator The residue is purified by preparative HPLC [Method 23] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Of the compound from Example 113A, 330 mg (1.15 mmol) in 12 ml of water/methanol 1:1 were admixed at RT with 279 mg (3.44 mmol) of potassium cyanate. The mixture was heated at 40° C. for 1 h and then admixed with 1.15 ml of 1M hydrochloric acid (1.15 mmol) and stirred overnight at RT. A further 93 mg (1.14 mmol) of potassium cyanate were added and the mixture was stirred further at RT for 3 h. The entire reaction mixture was purified by preparative HPLC [Method 10]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 292 mg (80% of theory) of the title compound. the mixture was stirred further at RT for 3 h The entire reaction mixture was purified by preparative HPLC [Method 10] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Of the compound from Example 113A, 330 mg (1.15 mmol) in 12 ml of water/methanol 1:1 were admixed at RT with 279 mg (3.44 mmol) of potassium cyanate. The mixture was heated at 40° C. for 1 h and then admixed with 1.15 ml of 1M hydrochloric acid (1.15 mmol) and stirred overnight at RT. A further 93 mg (1.14 mmol) of potassium cyanate were added and the mixture was stirred further at RT for 3 h. The entire reaction mixture was purified by preparative HPLC [Method 10]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 292 mg (80% of theory) of the title compound. the mixture was stirred further at RT for 3 h The entire reaction mixture was purified by preparative HPLC [Method 10] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: A solution of 330 mg (1.15 mmol) of the compound from Example 113A in 7 ml of pyridine was admixed at RT with 177 μl (2.29 mmol) of methanesulphonyl chloride. After 1 h the volatile constituents were removed on a rotary evaporator. The residue is purified by preparative HPLC [Method 23]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 312 mg (78% of theory) of the title compound. After 1 h the volatile constituents were removed on a rotary evaporator The residue is purified by preparative HPLC [Method 23] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV

Conditions: temp:40.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Of the compound from Example 113A, 330 mg (1.15 mmol) in 12 ml of water/methanol 1:1 were admixed at RT with 279 mg (3.44 mmol) of potassium cyanate. The mixture was heated at 40° C. for 1 h and then admixed with 1.15 ml of 1M hydrochloric acid (1.15 mmol) and stirred overnight at RT. A further 93 mg (1.14 mmol) of potassium cyanate were added and the mixture was stirred further at RT for 3 h. The entire reaction mixture was purified by preparative HPLC [Method 10]. The product fraction was freed from the solvents on a rotary evaporator. Drying of the residue in an HV gave 292 mg (80% of theory) of the title compound. the mixture was stirred further at RT for 3 h The entire reaction mixture was purified by preparative HPLC [Method 10] The product fraction was freed from the solvents on a rotary evaporator Drying of the residue in an HV