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Versatile solid-phase synthesis of secondary amines from alcohols. Development of an N-Boc-(o-nitrobenzene)sulfonamide linker |
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| Authors: | Miles S. CongreveCorinne Kay Jan J. ScicinskiSteven V. Ley Geoffrey WilliamsPeter J. Murray Stephen C. McKeownStephen P. Watson |
| Affiliation: | a GlaxoSmithKline, Cambridge Chemistry Laboratory, Lensfield Road, Cambridge CB2 1EW, UK b Department of Chemisty, Lensfield Road, Cambridge CB2 1EW, UK c OSI Pharmaceuticals, Watlington Road, Cowley, Oxfordshire OX4 6LT, UK d GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK |
| Abstract: | The development of a versatile amine releasing linker based on the modified o-nitrobenzene sulfonamide protective group is described. This new N-Boc-o-nitrobenzenesulfonamide (Boc-ONBS) linker enables the elaboration on resin of primary and secondary amines by sequential substitution of the sulfonamide moiety using the Mitsunobu reaction. A 16-member array of secondary and Boc protected primary amines was then prepared using this linker. |
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