| Identification | Back Directory | [Name]
Lazertinib | [CAS]
1903008-80-9 | [Synonyms]
CS-2767
GNS1480
YH25448
GNS-1480
Lazertinib
Lazertinib (YH25448)
Lazertinib(YH25448,GNS-1480)
YH 25448;YH25448;GNS-1480;GNS1480
LAZERTINIB; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480.
2-Propenamide, N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-4-methoxy-2-(4-morpholinyl)phenyl]- | [Molecular Formula]
C30H34N8O3 | [MDL Number]
MFCD31728331 | [MOL File]
1903008-80-9.mol | [Molecular Weight]
554.64 |
| Chemical Properties | Back Directory | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:6.5(Max Conc. mg/mL);11.72(Max Conc. mM) | [form ]
A solid | [pka]
12.39±0.70(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
RRMJMHOQSALEJJ-UHFFFAOYSA-N | [SMILES]
C(NC1=CC(NC2=NC=CC(N3C=C(CN(C)C)C(C4=CC=CC=C4)=N3)=N2)=C(OC)C=C1N1CCOCC1)(=O)C=C |
| Hazard Information | Back Directory | [Description]
Lazertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that is able to penetrate the central nervous system (CNS) and has been approved in South Korea for the treatment of patients with EGFR T790M mutation-positive non-small cell lung cancer (NSCLC) who have been previously treated with EGFR-TKIs. | [Uses]
Lazertinib is used in the preparation of heteroaryl pyrimidinylamine compounds for modulating EGFR mutant kinase activities. EGFR tyrosine-kinase inhibitor. | [Synthesis]
The construction of the second building block of lazertinib (22.7) began with a SNAr reaction between the aryl fluoride 22.4 and morpholine. The aniline nitrogen atom in 22.4 was formylated prior to nitro reduction. The newly formed aniline (22.5) underwent acylation with 3-chloropropionyl chloride (22.6) followed by a base-catalyzed elimination to afford the acrylate 22.7. Deprotonation of the N-formanilide prior to treatment with methyl sulfone 22.3 and subsequent exposure to aqueous sodium hydroxide promoted the binding of the 22.3 and 22.7 fragments and the simultaneous removal of the N-formyl group to afford the aminopyrimidine acrylate 22.8. Finally, a dimethylamino group was introduced via a STAB-H-mediated reductive amination to afford lazertinib (22) in high yield.
 | [IC 50]
EGFRT790M |
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| Company Name: |
CAREBIO PHARMA Gold
|
| Telephone: |
18501057619 18501057619 |
| Website: |
https://www.chemicalbook.com/supplier/25966678/ |
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