VHL Ligand 1 (hydrochloride) Synthesis Route

VHL Ligand 1 (hydrochloride) Synthesis

VHL Ligand 1 (hydrochloride) (Synonyms: (2S,4R)-1-((S)-2-Amino-3,3-dimethylbutanoyl)-4-hydroxy-N- (4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride)

VHL ligand 1 is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).1 It is the von Hippel-Lindau (VHL) E3 ligase binding portion of some VHL-based PROTACs, including BET PROTAC MZ1 (Item No. 21622).2

VHL Ligand 1 (hydrochloride)

A PROTAC building block

Item No. AB53900
CAS No. 1448189-80-7
Purity: 97%

100mg

＄27.00

250mg

＄33.00

＄104.00

＄405.00

10g

＄675.00

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VHL Ligand 1 (hydrochloride) Synthetic Route

AC64158

CAS: 68819-84-1

AB45102

CAS: 693-95-8

BA08222

CAS: 2308507-34-6

Av99903

CAS: 1448189-30-7

AB45674

CAS: 13726-69-7

AX07147

CAS: 1448191-54-5

BH87132

CAS: 1448189-45-4

Al54018

CAS: 62965-35-9

AY06994

CAS: 1448189-98-7

AB53900

CAS: 1448189-80-7

1: potassium acetate; palladium diacetate / N,N-dimethyl acetamide / 10 h / 150 °C / Inert atmosphere
2: hydrogenchloride / methanol
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / tetrahydrofuran / 2 h / 0 - 20 °C
4: hydrogenchloride / methanol
5: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 5 h / 20 °C
6: hydrogenchloride / methanol

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References

1.J.Med. Chem. 2021, 64, 10167−10184. 

2.Raina, K., Lu, J., Qian, Y., et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc. Natl. Acad. Sci. USA 113(26), 7124-7129 (2016).

3.Zengerle, M., Chan, K.-H., and Ciulli, A. Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem. Biol. 10(8), 1770-1777 (2015).