Synthesis of peptide-N-alkylamides on a new PS-TTEGDA polymer support using photolabile anchoring group
摘要:
Peptide-N-alkylamides were synthesised on a new highly solvating copolymer of 4% tetraethyleneglycol diacrylate-cross-linked polystyrene (PS-TTEGDA) support The polymer was synthesised by suspension polymerisation using a free radical initiator. The synthesis of C-terminal peptide-N-alkylamide involve prior incorporation of a photolabile linker, 3-nitro-4-bromo-methylbenzoic acid to the aminomethylated support The N-alkylamino group act as an anchoring group for the peptide as well as a latent function for the C-terminal modification of the attached peptide. Irradiation of the peptide-resin with 350 nm light in TFE/DCM resulted in the release of peptide-N-alkylamides. Synthetic utility of the new support was demonstrated by the synthesis of Boc-amino acid-N-alkylamides and C-terminal peptide-N-alkyl amides in 75-80% yields and with high purity. (C) 1999 Elsevier Science Ltd. All rights reserved.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY
申请人:Liu Hong
公开号:US20100234365A1
公开(公告)日:2010-09-16
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).