Triethylamine → (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-N-(5-methoxy-2-indolylcarbonyl)-4-piperidinamine

Participants

Reaction Steps

200 mg (0.550 mmol) of (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine are reacted in analogy to Example 4a with 126 mg (0.661 mmol) of 5-methoxyindole-2-carboxylic acid, 168 mg (0.661 mmol) of bis(2-oxo-3-oxazolidinyl)phosphinic chloride and 169 μl (1.21 mmol) of triethylamine. The title compound ##STR88## is obtained (118 mg, 41%) as white crystals of melting point 251° C. TLC: methylene chloride/methanol/conc. ammonia (2000:50: 1) Rf =0.81, FD-MS: M+ =535, 537; IR: 3440, 3280, 1625 cm-1.

Provenance & Evidence