Synthesis of n-substituted oligomers

Details Synthesis of n-substituted oligomers Synthesis of n-substituted oligomers

C - Chemistry, Metallurgy

07

K

C07K 14/00 (2006.01) A61K 31/00 (2006.01) A61K 38/04 (2006.01) A61K 38/16 (2006.01) A61K 49/00 (2006.01) C07C 237/42 (2006.01) C07C 243/24 (2006.01) C07C 259/06 (2006.01) C07C 281/00 (2006.01) C07D 295/13 (2006.01) C07K 1/04 (2006.01) C07K 5/04 (2006.01) C07K 7/04 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C08G 69/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2144067

A solid phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound .alpha.-haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, al- koxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displace- ment gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of di- verse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.

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