2-morpholin-4-ylbenzaldehyde

反応条件: temp:125.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A mixture of 2-fluorobenzaldehyde (0.5 mL, 4.8 mmol), morpholine (0.6 mL, 1.5 eq) and potassium carbonate (1.3 g, 2 eq) was heated in the microwave at 125° C. for 2.5 h. After evaporation, the residue was partitioned between water and DCM, the aqueous phase extracted with DCM. The combined organic phases were dried over sodium sulfate and concentrated in vacuo to afford 2-morpholinobenzaldehyde (0.57 g, 63%). After evaporation the residue was partitioned between water and DCM the aqueous phase extracted with DCM The combined organic phases were dried over sodium sulfate concentrated in vacuo

反応条件: temp:22.01; pressure:0.00; stir:

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

実験手順: Prepared by Procedure F and Scheme R using 2-(4-morpholinyl)benzaldehyde and 2-methyl-N-[3-(4-piperidinyl)phenyl]propanamide: ESMS m/e: 422.2 (M+H)+. Prepared by Procedure F and Scheme R

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

実験手順: Prepared by Procedure F and Scheme R using 2-(4-morpholinyl)benzaldehyde and 2-methyl-N-[3-(4-piperidinyl)phenyl]propanamide: ESMS m/e: 422.2 (M+H)+. Prepared by Procedure F and Scheme R

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

実験手順: Morpholinobenzaldehyde was reacted according to general procedure A using methanol/dioxane as a solvent. The product of this reaction was subsequently coupled with 4-aminomethyl benzonitrile according to general procedure B to give (RS)-N-(4-cyano-benzyl)-2-methoxy-2-(2-morpholin-4-yl-phenyl)-acetamide. Orange oil.

反応条件: temp:125.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: A mixture of 2-fluorobenzaldehyde (0.5 mL, 4.8 mmol), morpholine (0.6 mL, 1.5 eq) and potassium carbonate (1.3 g, 2 eq) was heated in the microwave at 125° C. for 2.5 h. After evaporation, the residue was partitioned between water and DCM, the aqueous phase extracted with DCM. The combined organic phases were dried over sodium sulfate and concentrated in vacuo to afford 2-morpholinobenzaldehyde (0.57 g, 63%). After evaporation the residue was partitioned between water and DCM the aqueous phase extracted with DCM The combined organic phases were dried over sodium sulfate concentrated in vacuo