The direct synthesis of the title amino acid derivatives from carboxylic esters and nitrones can be achieved in fair to good yields when lithium or magnesium ester enolates were treated with nitrones in THF at -78 °C or in Et2O at -20 to 0 °C, respectively. The products from the reaction of t-butyl acetate with 3,4-dihydroisoquinoline N-oxide or 5,5-dimethylpyrroline 1-oxide were transformed into (1,2,3,4-tetrahydroisoquinolin-1-ylidene)acetate or (pyrrolidin-2-ylidene)acetate derivatives in the presence of triphenylphosphine, carbon tetrachloride, and triethylamine in refluxing dichloromethane.

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Reaction of 2-(1-pyrrolyl)benzaldehyde with isocyanides in the presence of a catalytic amount of boron trifluoride diethyl etherate was followed by treatment with acetic anhydride in pyridine to give the corresponding O-acetyl derivatives of 4-alkyl(or aryl)aminopyrrolo[1,2-a]quinolin-5-ols in moderate yields.