Fig. 1: Design blueprint for the difunctionalization of BCBs to access 1,1,3-trisubstituted and 1,1,3,3-tetrasubstituted cyclobutanes enabled by remote C–H activation. | Nature Synthesis

Fig. 1: Design blueprint for the difunctionalization of BCBs to access 1,1,3-trisubstituted and 1,1,3,3-tetrasubstituted cyclobutanes enabled by remote C–H activation.

From: Difunctionalization of bicyclo[1.1.0]butanes enabled by merging C−C cleavage and ruthenium-catalysed remote C−H activation

Fig. 1

a, Selected drug molecules containing 1,3-difunctionalized cyclobutane skeleton. b, Current strategies50,51,52,53,54 for the synthesis of highly functionalized cyclobutanes via strain release. c, Our hypothesis on the 1,3-difunctionalization of BCBs by remote C−H activation to access valuable 1,1,3-trisubstituted and 1,1,3,3-tetrasubstituted cyclobutanes via a Ru-XAT process. Ar, aryl.; Het, heteroarenes.

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