2093386-36-6

Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.

Cereblon

[1] Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014 Aug 7;512(7512):49-53.??[Content Brief] DOI:10.1038/nature13527