ChemicalBook CAS DataBase List Selumetinib

Selumetinib synthesis

2synthesis methods

Product Name:Selumetinib
CAS Number:606143-52-6
Molecular formula:C17H15BrClFN4O3
Molecular Weight:457.68

Selumetinib was developed by AstraZeneca in the United Kingdom and is mainly used for the treatment of cholangiocarcinoma, colorectal cancer, and NSCLC. It can be synthesized by nitration, aminolysis, esterification, reduction, cyclization, methylation, hydrolysis and condensation from 2,3,4-trifluorobenzoic acid.

Methyl 4-Amino-3-Fluoro-5-Nitro-2-(Phenylamino)Benzoate

606093-58-7
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606143-52-6
307 suppliers
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Yield:-

Steps:

Multi-step reaction with 7 steps
1.1: palladium on activated charcoal; hydrogen / methanol; tetrahydrofuran / 5 h / 30 - 35 °C
1.2: 0.75 h / 10 - 20 °C
2.1: toluene-4-sulfonic acid / acetonitrile / 2.25 h / 20 - 65 °C
2.2: 0.5 h
2.3: 0.33 h / 45 - 50 °C
3.1: N-Bromosuccinimide / N,N-dimethyl-formamide / 1.17 h / 15 - 20 °C
4.1: N-chloro-succinimide / N,N-dimethyl-formamide / 42 h / 15 - 20 °C
5.1: sodium hydroxide; water / tetrahydrofuran / 12.17 h / 25 - 30 °C
6.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine / N,N-dimethyl-formamide / 0.17 h / 25 - 30 °C
6.2: 24 h / 25 - 30 °C
7.1: hydrogenchloride / water; ethanol / 24 h / 25 - 30 °C

References:

SUN PHARMACEUTICAL INDUSTRIES LIMITED;SAINI, Anil;KAZI, Muddassar Ajij;KHANNA, Mahavir Singh;PRASAD, Mohan WO2018/65924, 2018, A1

Methyl 5-(4-broMo-2-chlorophenylaMino)-4-fluoro-1-Methyl-1H-benzo[d]iMidazole-6-carboxylate

606144-02-9
51 suppliers
$505.22/5MG

606143-52-6
307 suppliers
$25.00/10mg

References

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