Triphenylphosphine → benzyl N-[4-[[[2-[2,6-difluoro-4-(2-morpholin-4-ylethoxy)phenyl]-2-ethoxyacetyl]amino]methyl]benzenecarboximidoyl]carbamate

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Reaction Steps

To a mixture of (RS)-[(4-{[2-(2,6-difluoro-4-hydroxy-phenyl)-2-ethoxy-acetylamino]-methyl}-phenyl)-imino-methyl]-carbamic acid benzyl ester (100 mg), N-(2-hydroxyethyl)morpholine (29 mg) and polymer bound triphenylphosphine (˜3 mmol/g, 167 mg) in CH2Cl2 (2 ml) was added di-tert-butyl azodicarboxylate (93 mg) before shaking 22 h at rt. After filtration of the polymer the solvent was evaporated and the residue was purified by HPLC to obtain 28 mg of (23%) (RS)-{[4-({2-[2,6-difluoro-4-(2-morpholin-4-yl-ethoxy)-phenyl]-2-ethoxy-acetylamino}-methyl)-phenyl]-imino-methyl}-carbamic acid benzyl ester.

Provenance & Evidence