4-Methylmorpholine → HCID 86585062, compound

Participants

Reaction Steps

(al) 150 mg (0.4 mmol) (2S,4R)-4-Acetylsulfanyl-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carboxylic acid in 10 ml CH2Cl2 were treated with 49 μl (0.43 mmol, 1.1 eq) 4-methyl morpholine, 142 mg (0.47 mmol, 1.2 eq) TPTU and 140 mg (0.59 mmol, 1.5 eq) 4-(methyl-methylaminoacetyl-amino)-benzoic acid methyl ester. The solution was stirred at RT over night. The mixture was concentrated and purified by flash chromatography yielding 233 mg (98%) (2S,4R)-4-[[[[4-Acetylsulfanyl-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]-amino]-acetyl]-methyl-amino]-benzoic acid methyl ester as white foam, MS: 598 (MH+).

Provenance & Evidence