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. 2020 Oct 30;1(5):273–312. doi: 10.37349/etat.2020.00018

Figure 11.

Figure 11.

Use of triazoles in library synthesis. A. Azide intermediate 59 was reacted with alkynes bearing warheads for CRBN or VHL to afford two series of triazole-containing PROTACs 60 and 61 with variable linker lengths; B. amino azide intermediate 62 was conjugated to various anchors and reacted with alkyne derivatives of niraparib (63) or olaparib (64) to screen different warhead/anchor combinations. This identified potent MDM2-recruiting PROTAC 65