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PyAOP is a phosphonium salt used as a coupling reagent in Solid-phase peptide synthesis, without undergoing side reactions with the amino terminus. PyAOP is a derivative of HOAt.
2. Peptide bond-forming reagents HOAt and HATU are not mutagenic in the bacterial reverse mutation test
John Nicolette, Robin E Neft, Jessica Vanosdol, Joel Murray Environ Mol Mutagen. 2016 Apr;57(3):236-40. doi: 10.1002/em.21997. Epub 2016 Feb 3.
The peptide bond-forming reagents 1-hydroxy-7-azabenzotriazole (HOAt, CAS 39968-33-7) and O-(7-Azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (HATU, CAS 148893-10-1) either have structural alerts, unclassified features or are considered out of domain when evaluated for potential mutagenicity with in silico programs DEREK and CaseUltra. Since they are commonly used reagents in pharmaceutical drug syntheses, they may become drug substance or drug product impurities and would need to be either controlled to appropriately safe levels or tested for mutagenicity. Both reagents were tested in the bacterial reverse mutation (Ames) test at Covance, under GLP conditions, following the OECD test guideline and ICH S2(R1) recommendations and found to be negative. Our data show that HOAt and HATU-common pharmaceutical synthesis reagents-are not mutagenic, and can be treated as ordinary drug impurities.
![(3-Hydroxy-3H-1,2,3-triazolo[4,5-b]pyridinato-O)tri-1-pyrrolidinylphosphonium hexafluorophosphate](https://resource.bocsci.com/structure/156311-83-0.gif)
