HATU

A peptide coupling reagent.

Mineral resources prospecting by synthetic application of TM/ETM+, Quickbird and Hyperion data in the Hatu area, West Junggar, Xinjiang, China.[Pubmed:26911195]

Sci Rep. 2016 Feb 25;6:21851.

The HATU area, West Junggar, Xinjiang, China, is situated at a potential gold-copper mineralization zone in association with quartz veins and small granitic intrusions. In order to identify the alteration zones and mineralization occurrences in this area, the Landsat Thematic Mapper (TM) and Enhanced Thematic Mapper (ETM+), Quickbird, Hyperion data and laboratory measured spectra were combined in identifying structures, alteration zones, quartz veins and small intrusions. The hue-saturation-intensity (HSI) color model transformation was applied to transform principal component analysis (PCA) combinations from R (Red), G (Green) and B (Blue) to HSI space to enhance faults. To wipe out the interference of the noise, a method, integrating Crosta technique and anomaly-overlaying selection, was proposed and implemented. Both Jet Propulsion Laboratory Spectral Library spectra and laboratory-measured spectra, combining with matched filtering method, were used to process Hyperion data. In addition, high-resolution Quickbird data were used for unraveling the quartz veins and small intrusions along the alteration zones. The Baobei fault and a SW-NE-oriented alteration zone were identified for the first time. This study eventually led to the discovery of four weak gold-copper mineralized locations through ground inspection and brought new geological knowledge of the region's metallogeny.

Evaluation of combined use of Oxyma and HATU in aggregating peptide sequences.[Pubmed:28139012]

J Pept Sci. 2017 Apr;23(4):272-281.

Polypeptides are finding increasing applications as therapeutics because of their specificity that often translates into excellent safety, tolerability, and efficacy profiles in humans. New synthetic methodologies for their preparation are thereby continuously sought to reduce the costs associated to chain assembly and purification. Although solid-phase peptide synthesis has become one of the most advanced synthetic procedures at both laboratory and industrial scale, the process is often complicated by aggregation phenomena originating from the combined occurrence of intermolecular and intramolecular hydrogen bonding, hydrophobic interactions, or other effects. Altogether, these effects cause accumulation of many side products and synthetic mixtures extremely hard to separate and purify, strongly affecting the costs of the final material. In the attempt to optimize the coupling steps of some well-known aggregating or otherwise difficult to obtain peptides, we have comparatively investigated the use of Oxyma/DIC and HATU/Sym-collidine as second coupling reagents in double coupling settings for the preparation of some model peptides. Comparative analytical data obtained on the unpurified products with the two different protocols clearly show that the use of Oxyma/DIC largely improves the content of the target molecules in the final crude materials, making the synthesis more convenient and cost-effective. Copyright (c) 2017 European Peptide Society and John Wiley & Sons, Ltd.

Peptide bond-forming reagents HOAt and HATU are not mutagenic in the bacterial reverse mutation test.[Pubmed:26840011]

Environ Mol Mutagen. 2016 Apr;57(3):236-40.

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.

Rapid HATU-mediated solution phase siRNA conjugation.[Pubmed:21744777]

Bioconjug Chem. 2011 Aug 17;22(8):1723-8.

Conditions for facile solution-phase amide conjugation of amine-modified siRNA with a diverse set of carboxylic acid partners using the coupling reagent HATU are described. These conditions eliminate the need for isolated activated esters and allow for rapid access to conjugates with a wide range of lipophilicity and functionality in good yield.