1-Methylpiperazin-2-one → {(S)-6-[(R)-4-(4-Methyl-3-oxo-piperazin-1-ylmethyl)-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid

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Reaction Steps

The methyl ester of the title compound, {(S)-6-[(R)-4-(4-methyl-3-oxo-piperazin-1-ylmethyl)-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester, is prepared from {(S)-6-[(R)-4-bromomethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester and 1-methyl-piperazin-2-one following a procedure analogous to that described for Intermediate 42. The crude product is directly submitted to the saponification conditions described for Example 1 to give the title compound upon chromatography on reversed phase (HPLC; acetonitrile/water). LC (method 6): tR=1.03 min; Mass spectrum (ESI+): m/z=505 [M+H]+.

Provenance & Evidence