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

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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 106 mg (0.661 mmol) of indole-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 ##STR87## is obtained (89 mg, 32%) as white crystals with melting point 254° C. TLC: methylene chloride/methanol/conc. ammonia (2000:50:1) Rf =0.56, FD-MS: M+ =505, 507; IR: 3430, 3290, 1625 cm-1.

Provenance & Evidence