Asandeutertinib

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Asandeutertinib, Osimertinib-d3

CAS 1638281-46-5

9EKD2E8BM5
N-(2-(2-(dimethylamino)ethyl-methylamino)-4-methoxy-5-((4-(1-(trideuteriomethyl)indol-3-yl)pyrimidin-2-yl)amino)phenyl)prop-2-enamide
N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-[1-(trideuteriomethyl)indol-3-yl]pyrimidin-2-yl]amino]phenyl]prop-2-enamide

N-[2-{2-(dimethylamino)ethylamino}-4-methoxy-5-({4-[1-(2H3)methyl-1H-indol-3-yl]pyrimidin-2-
yl}amino)phenyl]prop-2-enamide
epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, antineoplastic

MF C28H30. 2H3. N7O2, C₂₈H₃₀D₃N₇O₂ MW 502.6 g/mol

Asandeutertinib is an investigational new drug that is being evaluated for the treatment of cancer. It is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with antineoplastic properties.^[1][2] Developed by TYK Medicines, this small molecule drug is currently being investigated for the treatment of non-small cell lung cancer (NSCLC), particularly in patients with EGFR mutations.^[1][3]

PAT

2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereofPublication Number: US-10414756-B2Priority Date: 2014-08-15Grant Date: 2019-09-17
2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereofPublication Number: US-2018016258-A1Priority Date: 2014-08-15

SYN

[US10414756]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US210080627&_cid=P21-MFT3HT-86141-1

Embodiment 3A

N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-(D₃-methyl)indol-3-yl)pyrimidin-2-yl]amino}phenyl)-2-acrylamide

Under ice bath condition, to N ¹-(2-dimethylaminoethyl)-5-methoxy-N ¹-methyl-N ⁴-[4-(1-[D ₃-methylindol]-3-yl)pyrimidin-2-yl]phenyl-1,2,4-triamine (intermediate 3, 20 g) in THF (200 mL) and water (20 mL), was added 6.9 g NaOH. Acryloyl chloride 4.05 g was added while stirring, the reaction mixture was stirred for 30 min at room temperature, then stirred for 1 h at room temperature. After the result of TLC showed that the reaction was complete, 200 mL water and 20 mL aqueous ammonia were added into the reaction mixture, the solid was precipitated and filtered out. The solid was collected and washed with water, dried for 8 h at 50° C. to deliver the title compound (yield 87%).

¹H-NMR: 2.70 (3H, s), 2.88 (6H, d), 3.35 (4H, s), 3.92 (3H, s), 5.77 (1H, d), 6.27 (1H, d), 6.67 (1H, dd), 7.04-7.25 (2H, m), 7.28 (1H, t), 7.46 (1H, d), 7.59 (1H, d), 8.23 (2H, s), 8.85 (1H, s), 9.45 (1H, s), 9.55 (1H, s).

ESI+: [M+H ⁺] 503.29.

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References

“Asandeutertinib”. PatSnap.
“Asandeutertinib”. IUPHAR/BPS Guide to PHARMACOLOGY.
Han B, Zhang W, Wu L, Chen B, Zhao Y, Liu J, et al. (October 2024). “P1. 12A. 07 A Phase 1 Study of TY-9591 in Advanced Non-Small Cell Lung Cancer (NSCLC) Patients with EGFR Positive Mutation”. Journal of Thoracic Oncology. 19 (10): S195. doi:10.1016/j.jtho.2024.09.353.

Clinical data

Other names	Runnor-9591, TY 9591
Identifiers
IUPAC name
CAS Number	1638281-46-5
PubChem CID	87056175
IUPHAR/BPS	13201
ChemSpider	129431787
UNII	9EKD2E8BM5
Chemical and physical data
Formula	C₂₈H₃₀D₃N₇O₂
Molar mass	502.636 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

////////////Asandeutertinib, antineoplastic, 9EKD2E8BM5, Osimertinib-d3