Synthesis of a sulfahydantoin library.
A five-step solid-phase synthesis of sulfahydantoins from alpha-amino acids and aldehydes was developed. The synthetic method allows the use of hindered amino acids, including Val, Phg, and Aib, and use of aromatic aldehydes substituted with electron-withdrawing and -donating groups. Some limitations were encountered with amino acids with reactive side chains. A small but diverse library of compounds was produced for biological testing.
Albericio
F
F
Department of Organic Chemistry, University of Barcelona, 08028-Barcelona, Spain.
Bryman
L M
LM
Garcia
J
J
Michelotti
E L
EL
Nicolás
E
E
Tice
C M
CM
D000447:Aldehydes / Q000737:chemistry; D000596:Amino Acids / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques; D006827:Hydantoins / Q000138:chemical synthesis*; D015394:Molecular Structure; D013056:Spectrophotometry, Ultraviolet; D013457:Sulfur Compounds / Q000138:chemical synthesis*; D013844:Thiazoles / Q000737:chemistry*
D000447:Aldehydes; D000596:Amino Acids; D006827:Hydantoins; D013457:Sulfur Compounds; D013844:Thiazoles