Acetic Acid → [(6R,7S)-2-fluoro-6-methyl-9-(2-morpholin-4-yl-ethyl)-8-oxo-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-yl]-carbamic acid tert-butyl ester

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Reaction Steps

0.10 mg (0.28 mmol) [(6R,7S)-2-Fluoro-6-methyl-8-oxo-9-(2-oxo-ethyl)-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-yl]-carbamic acid tert-butyl ester in 4 ml methanol was reacted with 0.036 ml (0.40 mmol) morpholine, 0.07 ml acetic acid and 0.03 g sodium cyanoborohydride at room temperature. Chromatography on silicagel with ethylacetate/heptane 1:1 yielded 0.09 g (73%) [(6R,7S)-2-fluoro-6-methyl-9-(2-morpholin-4-yl-ethyl)-8-oxo-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-yl]-carbamic acid tert-butyl ester, MS m/e (%): 424.3 (M+H+, 100).

Provenance & Evidence