Lithium Hydroxide → {(S)-1-tert-Butoxycarbonyl-4-[2-(3-fluoro-2-methyl-benzyl)-1-phenyl-indolizine-3-carbonyl]-piperazin-2-yl}-acetic acid

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Reaction Conditions

Reaction Steps

To a solution of the compound of step 4 (1.40 g, 2.33 mmol) in 15.5 ml of dioxane was added 3.5 ml of a 1 M aqueous solution of lithium hydroxide and the mixture was heated at 50° C. for 1 h. The solvents were evaporated under reduced pressure and the residue was dissolved in 45 ml of water. The solution was cooled to 0° C. and acidified to pH 2 with 5 N hydrochloric acid. The obtained suspension was extracted with EA and the combined organic phases were washed with brine, dried over sodium sulfate, filtered and evaporated to dryness. 1.37 g of the title compound were obtained as a green solid melting at 103-105° C.

Provenance & Evidence