Morpholine → 2-(Tert-butoxycarbonylamino)indan-5-carboxylic acid morpholinamide

Participants

Reaction Steps

Using 2-(tert-butoxycarbonylamino)-5-carboxyindan (1.01 g, 3.6 mmol), morpholine (0.48 ml, 5.5 mmol), triethylamine (3.6 ml, 26 mmol), propanephosphonic acid anhydride (5.3 ml), dimethylaminopyridine (a catalytic amount) and methylene chloride (27 ml), a similar procedure to a) in Example 29 was carried out. The product obtained was purified by silica gel chromatography (methylene chloride:methanol=95:5) to obtain 2-(tert-butoxycarbonylamino)indan-5-carboxylic acid morpholinamide (1.0 g, 2.9 mmol) having the following physical properties:

Provenance & Evidence