Trifluoroacetic acid methylene chloride → HCID 18689598, compound

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The above-described cyclized products 4-{[2-(4-cyano-phenyl)-2-(3-cyclohexylmethyl-1,4-dioxo-1,3,4,6,11,11a-hexahydro-pyrazino[1,2-b]isoquinolin-2-yl)-acetylamino]-methyl}-benzoic acid tert-butyl ester (diastereomers A and B) were treated with a 1:1 CH2Cl2 /CF3CO2H solution according to General Method 3 to afford 27 mg (100%) of 4-{[2-(4-cyano-phenyl)-2-(3-cyclohexylmethyl-1,4-dioxo-1,3,4,6,11,11a-hexahydro-pyrazino[1,2-b]isoquinolin-2-yl)-acetylamino]-methyl}-benzoic acid (diastereomer A) and 35 mg (100%) of 4-{[2-(4-cyano-phenyl)-2-(3-cyclohexylmethyl-1,4-dioxo-1,3,4,6,11,11a-hexahydro-pyrazino[1,2-b]isoquinolin-2-yl)-acetylamino]-methyl}-benzoic acid (diastereomer B).

Provenance & Evidence