AZD 3264 an IKK2 Inhibitor from Astra Zeneca

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New Drug Approvals

Figure

AZD 3264

MW 441.50

CAS 1609281-86-8

MF C21 H23 N5 O4 S
3-​Thiophenecarboxamide​, 2-​[(aminocarbonyl)​amino]​-​5-​[4-​(3,​5-​dimethyl-​4-​isoxazolyl)​-​2-​[(3S)​-​3-​pyrrolidinyloxy]​phenyl]​-
2-(Carbamoylamino)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[(3S)-pyrrolidin-3-yloxy]phenyl]thiophene-3-carboxamide

Inhibition of IkB-kinase IKK2 has been identified as one of the novel pathways to treat inflammatory conditions such as asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis

Astrazeneca Ab,

……………………..

PATENT

WO 2003010158

https://www.google.com/patents/WO2003010158A1?cl=en

Figure

The synthesis began with the aromatic nucleophilic substitution reaction of 2-fluorobromobenzene (2) with (S)-N-Boc-3-pyrrolidinol 3 to give the bromo intermediate 4, which was borylated via halogen metal exchange using n-hexLi in THF followed by treatment with triisopropyl borate and acidic work-up to give the boronic acid intermediate 5. Suzuki coupling of the boronic acid 5 with bromothiophene 6(2)afforded the intermediate 7. Intermediate 7 was subjected to regioselective bromination using bromine in acetic acid. This reaction was nonregioselective and yielded 17% of the required…

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