title: Solid phase organic synthesis (SPOS): a novel route to diketopiperazines and diketomorpholines.
abstract: The solid phase synthesis of libraries containing a 1,3,4,6-tetrasubstituted-2,5-diketo-1,4-piperazine scaffold (DKP) or a 3,4,6-trisubstituted-2,5-diketo-1,4-morpholine scaffold (DKM) from alpha-bromocarboxylic acids and amines is described. Using a design strategy which we refer to as divergent library design, both templates were prepared from a common intermediate. The general utility of this synthetic route in creating novel, non-peptidyl chemical libraries is discussed.
authors.affiliation: Chiron Corporation, Emeryville, CA 94806, USA.
authors.forename: B O
authors.initials: BO
authors.lastname: Scott
authors.forename: A C
authors.initials: AC
authors.lastname: Siegmund
authors.forename: C K
authors.initials: CK
authors.lastname: Marlowe
authors.forename: Y
authors.initials: Y
authors.lastname: Pei
authors.forename: K L
authors.initials: KL
authors.lastname: Spear
mesh_terms: D002625:Chemistry, Organic; D002851:Chromatography, High Pressure Liquid; D019020:Directed Molecular Evolution / Q000379:methods*; D015195:Drug Design; D008722:Methods; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry; D055601:Organic Chemistry Phenomena; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry; D012117:Resins, Synthetic
chemical_list: D009025:Morpholines; D010879:Piperazines; D012117:Resins, Synthetic