271576-76-2Relevant articles and documents
Deprotection of N-Boc Groups under Continuous-Flow High-Temperature Conditions
Li, Bryan,Li, Ruizhi,Dorff, Peter,McWilliams, J. Christopher,Guinn, Robert M.,Guinness, Steven M.,Han, Lu,Wang, Ke,Yu, Shu
, p. 4846 - 4855 (2019/01/30)
The scope of thermolytic, N-Boc deprotection was studied on 26 compounds from the Pfizer compound library, representing a diverse set of structural moieties. Among these compounds, 12 substrates resulted in clean (≥95% product) deprotection, and an additional three compounds gave ≥90% product. The thermal de-Boc conditions were found to be compatible with a large number of functional groups. A combination of computational modeling, statistical analysis, and kinetic model fitting was used to support an initial, slow, and concerted proton transfer with release of isobutylene, followed by a rapid decarboxylation. A strong correlation was found to exist between the electrophilicity of the N-Boc carbonyl group and the reaction rate.
SUBSTITUTED PYRAZOLES AS P38 KINASE INHIBITORS
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, (2008/06/13)
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SUBSTITUTED PYRAZOLES AS P38 KINASE INHIBITORS
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, (2008/06/13)
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