| abstract |
The present invention relates to building units suitable for the synthesis of backbone cyclized peptides. The building units of this invention have structures of the formula (I): X-AAm-U-AAp-Y wherein AAm and AAp are residues of natural or synthetic amino acids and U is C.alpha.ON¢(CH2)n+1W! or (C.alpha.H2N)¢CO(CH2)qW!, in which C.alpha. is a carbon atom and is the .alpha. carbon of AAm if m > 0. W is NH-X or COY, and X is H, Boc, Z, Fmoc, or Alloc while Y is the hydroxyl group of a carboxylic acid moiety or a carboxylic acid protecting group. The letter m refers to an integer from 0 to 10; n is a number from 0 to 6; p is a number from 1 to 10; and q is a number from 1 to 6. The present invention is also directed to methods of synthesizing building units of formula (I) via different routes. |