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Metal Hydride? NO Protection, NO Problem and NO-Where to Hide

Process chemists at Genentech recently published their work on development of a kilo-scale synthesis of JAK-1 inhibitor- GDC-4379 (Figure 1).1The central heterocyclic core of the molecule consists of a 4-aminopyrazole moiety (elaborated as the pyrazolopyrimidene amide- presumably the inhibitor hinge binding fragment in the kinase active site) with an additional aryl substituent at C-3 and

Breaking up is hard to do

As synthetic chemists we are very familiar with making chemical bonds, particularly C-C bonds, and building complex molecules. Having said that, fundamentally, with sufficient energy and entropy in the driving seat, it should be quicker and easier to break molecules apart. Deconstructive processes are not, however, as common as one might think- particularly cleavage of

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