N'-羟基-3-甲氧基-丙脒

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

实验步骤: 300 mg (0.69 mmol) of the compound from Example 37A and 246 mg (2.08 mmol) of N′-hydroxy-3-methoxypropanimidamide were initially charged in 2.6 ml of DMF and reacted with 396 mg (1.0 mmol) of HATU and 0.36 ml (269 mg, 2.1 mmol) of N,N-diisopropylethylamine. The reaction mixture was stirred at RT for 15 minutes and then partitioned between water and ethyl acetate. The organic phase was washed repeatedly with water, dried over sodium sulphate and concentrated under reduced pressure. The residue was dissolved in 2.0 ml of DMF and converted in a microwave at 180° C. for 2 minutes. The reaction mixture was purified by means of preparative HPLC. Yield: 141 mg (38% of theory) partitioned between water and ethyl acetate The organic phase was washed repeatedly with water dried over sodium sulphate concentrated under reduced pressure The residue was dissolved in 2.0 ml of DMF converted in a microwave at 180° C. for 2 minutes The reaction mixture was purified by means of preparative HPLC

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

实验步骤: According to General Method 6A, 153 mg (0.270 mmol, purity 50%) of the compound from Example 59A and 41.3 mg (0.297 mmol, purity 85%) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 46.6 mg (32% of theory, purity 72%) were reacted Yield: 46.6 mg (32% of theory, purity 72%)

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

实验步骤: According to General Method 6A, 300 mg (0.720 mmol) of the compound from Example 45A and 93.6 mg (0.792 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 231 mg (63% of theory, approx. 15% trans isomer) were reacted Yield: 231 mg (63% of theory, approx. 15% trans isomer)

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

实验步骤: According to General Method 6A, 600 mg (1.43 mmol) of the compound from Example 25A and 232 mg (1.58 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 398 mg (53% of theory) were reacted Yield: 398 mg (53% of theory)

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

实验步骤: According to General Method 6A, 600 mg (1.491 mmol) of the compound from Example 16A and 242 mg (1.640 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 350 mg (46% of theory) were reacted Yield: 350 mg (46% of theory)

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

实验步骤: According to General Method 6A, 300 mg (0.828 mmol) of the compound from Example 7A and 134 mg (0.910 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 185 mg (49% of theory) were reacted Yield: 185 mg (49% of theory)

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

实验步骤: 300 mg (0.69 mmol) of the compound from Example 37A and 246 mg (2.08 mmol) of N′-hydroxy-3-methoxypropanimidamide were initially charged in 2.6 ml of DMF and reacted with 396 mg (1.0 mmol) of HATU and 0.36 ml (269 mg, 2.1 mmol) of N,N-diisopropylethylamine. The reaction mixture was stirred at RT for 15 minutes and then partitioned between water and ethyl acetate. The organic phase was washed repeatedly with water, dried over sodium sulphate and concentrated under reduced pressure. The residue was dissolved in 2.0 ml of DMF and converted in a microwave at 180° C. for 2 minutes. The reaction mixture was purified by means of preparative HPLC. Yield: 141 mg (38% of theory) partitioned between water and ethyl acetate The organic phase was washed repeatedly with water dried over sodium sulphate concentrated under reduced pressure The residue was dissolved in 2.0 ml of DMF converted in a microwave at 180° C. for 2 minutes The reaction mixture was purified by means of preparative HPLC

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

实验步骤: According to General Method 6A, 153 mg (0.270 mmol, purity 50%) of the compound from Example 59A and 41.3 mg (0.297 mmol, purity 85%) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 46.6 mg (32% of theory, purity 72%) were reacted Yield: 46.6 mg (32% of theory, purity 72%)

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

实验步骤: According to General Method 6A, 300 mg (0.720 mmol) of the compound from Example 45A and 93.6 mg (0.792 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 231 mg (63% of theory, approx. 15% trans isomer) were reacted Yield: 231 mg (63% of theory, approx. 15% trans isomer)

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

实验步骤: According to General Method 6A, 600 mg (1.43 mmol) of the compound from Example 25A and 232 mg (1.58 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 398 mg (53% of theory) were reacted Yield: 398 mg (53% of theory)

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

实验步骤: According to General Method 6A, 600 mg (1.491 mmol) of the compound from Example 16A and 242 mg (1.640 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 350 mg (46% of theory) were reacted Yield: 350 mg (46% of theory)

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

实验步骤: According to General Method 6A, 300 mg (0.828 mmol) of the compound from Example 7A and 134 mg (0.910 mmol) of N′-hydroxy-3-methoxypropanimidamide were reacted Yield: 185 mg (49% of theory) were reacted Yield: 185 mg (49% of theory)