53843-54-2Relevant academic research and scientific papers
Synthesis of orthogonally protected optically pure ketopiperazine, diketopiperazine, ketodiazepane, and 3-aminopyrrolidone building blocks for peptidomimetic combinatorial chemistry
Gellerman, Gary,Hazan, Eran,Kovaliov, Marina,Albeck, Amnon,Shatzmiler, Shimon
experimental part, p. 1389 - 1396 (2009/04/10)
A simple and convenient synthesis of orthogonally protected multi-tethered, optically pure 2-ketopiperazine, diketopiperazine, 2-ketodiazepane and 3-aminopyrrolidone scaffolds for Fmoc combinatorial chemistry has been developed. It utilizes accessible chi
HETEROCYCLIC SCAFFOLDS USEFUL FOR PREPARATION OF COMBINATORIAL LIBRARIES, LIBRARIES AND METHODS OF PREPARATION THEREOF
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Page/Page column 28, (2009/04/25)
Disclosed are heterocyclic scaffolds useful, for example, for solid-phase organic synthesis of combinatorial libraries and methods for the preparation thereof. Also disclosed are libraries, including combinatorial libraries, and methods for preparation thereof. Exemplified are the following scaffolds (I):
Protected Lactam-Bridged Dipeptides for Use as Conformational Constraints in Peptides
Freidinger, Roger M.,Perlow, Debra Schwenk,Veber, Daniel F.
, p. 104 - 109 (2007/10/02)
General methods have been devised for the synthesis of lactam-constrained dipeptide analogues having five-, six-, and seven-membered rings.Three different paths from protected chiral α-amino acids to lactams involving intramolecular alkylation, intramolecular acylation, and insertion of a one carbon unit by condensation with formaldehyde have been utilized.The first two methods produce chiral products stereospecifically, but considerable racemization occurs in the third route which leads to a 4-oxo-5-amino-1,3-thiazine (13).The products are prepared in good yield and have protecting groups making them suitable for incorporation into higher peptides by methods commonly used.
