Safety as a Factor in Reaction Development: Considerations of Sensitization Potential with Amide Bond Forming Reagents
In response to an increased awareness of sensitization issues with amide bond forming agents, a detailed toxicological analysis of this broad family of reagents was undertaken which led to a quantitative ranking of the sensitization potential of these commonly used compounds. This data enables occup...
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| Published in | Helvetica chimica acta Vol. 106; no. 11 |
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| Main Authors | , , |
| Format | Journal Article |
| Language | English |
| Published |
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01.11.2023
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| Abstract | In response to an increased awareness of sensitization issues with amide bond forming agents, a detailed toxicological analysis of this broad family of reagents was undertaken which led to a quantitative ranking of the sensitization potential of these commonly used compounds. This data enables occupational toxicologists to guide the safer use of these reagents in the laboratory, but it also provides an opportunity for chemists working on reaction development, optimization and scale‐up. To illustrate this, one of the strongest sensitizers, EDAC, is compared with the performance of one of the weakest, TCFH, showing the potential of this data for minimizing risks for researchers when using this family of reagents. |
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| AbstractList | In response to an increased awareness of sensitization issues with amide bond forming agents, a detailed toxicological analysis of this broad family of reagents was undertaken which led to a quantitative ranking of the sensitization potential of these commonly used compounds. This data enables occupational toxicologists to guide the safer use of these reagents in the laboratory, but it also provides an opportunity for chemists working on reaction development, optimization and scale-up. To illustrate this, one of the strongest sensitizers, EDAC, is compared with the performance of one of the weakest, TCFH, showing the potential of this data for minimizing risks for researchers when using this family of reagents.
image In response to an increased awareness of sensitization issues with amide bond forming agents, a detailed toxicological analysis of this broad family of reagents was undertaken which led to a quantitative ranking of the sensitization potential of these commonly used compounds. This data enables occupational toxicologists to guide the safer use of these reagents in the laboratory, but it also provides an opportunity for chemists working on reaction development, optimization and scale‐up. To illustrate this, one of the strongest sensitizers, EDAC, is compared with the performance of one of the weakest, TCFH, showing the potential of this data for minimizing risks for researchers when using this family of reagents.To Professor Scott Denmark on his 70th Birthday In response to an increased awareness of sensitization issues with amide bond forming agents, a detailed toxicological analysis of this broad family of reagents was undertaken which led to a quantitative ranking of the sensitization potential of these commonly used compounds. This data enables occupational toxicologists to guide the safer use of these reagents in the laboratory, but it also provides an opportunity for chemists working on reaction development, optimization and scale‐up. To illustrate this, one of the strongest sensitizers, EDAC, is compared with the performance of one of the weakest, TCFH, showing the potential of this data for minimizing risks for researchers when using this family of reagents. |
| Author | Beutner, Gregory L. Williams, Michael J. George, David T. |
| Author_xml | – sequence: 1 givenname: David T. surname: George fullname: George, David T. organization: Bristol Myers Squibb Company – sequence: 2 givenname: Michael J. surname: Williams fullname: Williams, Michael J. organization: Bristol Myers Squibb Company – sequence: 3 givenname: Gregory L. orcidid: 0000-0001-8779-1404 surname: Beutner fullname: Beutner, Gregory L. email: gregory.beutner@bms.com organization: Bristol Myers Squibb Company |
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| Cites_doi | 10.1787/9789264090958-en 10.1021/acscombsci.6b00103 10.1080/00397918608076318 10.1002/chem.202005351 10.1111/j.1600-0536.1995.tb00635.x 10.1016/j.yrtph.2009.08.016 10.1021/acs.chemrestox.2c00031 10.1021/acs.joc.9b03280 10.1016/S0040-4020(99)00809-1 10.1021/acs.oprd.9b00140 10.1021/cr100048w 10.1787/9789264071100-en 10.1111/j.1600-0536.2009.01685.x 10.1039/b602413k 10.1016/j.bmcl.2006.11.020 10.1787/9789264067318-en 10.1111/j.0105-1873.2005.0483i.x 10.1021/acs.chas.0c00025 10.1007/s12039-015-0988-6 10.1021/acs.orglett.3c01611 10.1111/j.0105-1873.2003.0128h.x 10.1021/ol401677a 10.1021/jo00349a028 10.1016/S0040-4020(01)90369-2 10.1787/9789264264618-en 10.1021/ja00902a036 10.1021/jo302324r 10.1021/acs.orglett.8b01591 10.1021/ol802946p 10.1787/9789264076303-en 10.1016/S0040-4020(01)80993-5 10.1021/acs.oprd.8b00193 10.1021/acs.joc.1c01427 10.1111/j.1600-0536.1975.tb05374.x |
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| Keywords | toxicology PEPTIDE COUPLING REAGENTS ALLERGIC CONTACT-DERMATITIS amides heterocycles carbodiimide HATU |
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| Title | Safety as a Factor in Reaction Development: Considerations of Sensitization Potential with Amide Bond Forming Reagents |
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