* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
With hydrogenchloride; In 1,4-dioxane; ethyl acetate;
General procedure: A solution of compound 27 (12 mmol), aldehyde (12 mmol) and piperidine (3.6 mmol) in MeOH (60 mL) was stirred at rt. overnight, remove solvent under vacuum, the residue was purified by flash column chromatography (Hexane/EA = 8/1) to give a white solid, which was subject to Boc deprotection conditions in ethyl acetate (30 mL) by 4 M HC1 in dioxane (15 mL), the solution to give 28-36 as white solid.
2
[ 1449240-68-9 ]
[ 1449240-30-5 ]
Yield
Reaction Conditions
Operation in experiment
With palladium 10% on activated carbon; hydrogen; In methanol; at 20.0℃;
A mixture of compound 31 (KLIII016) (100 mg) and 10% Pd/C (50 mg) in methanol (15 mL) was hydrogenated at rt. overnight, suction filter to remove the catalyst, the filtrate was concentrated under vacuum, then ethyl acetate (ImL) was added, suction filter, and washed with ethyl acetate to give a white solid.