2-Amino-5-bromo-4-methoxypyrimidine → 5-bromo-N-[2-fluoro-5-(trifluoromethyl)phenyl]-4-methoxypyrimidin-2-amine

HRID 665

Reaction equation

HRID 665 reaction equation
COc1nc(N)ncc1Br.Fc1ccc(C(F)(F)F)cc1I>CC(=O)O.CC(=O)O.Cc1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1coc(P(c2ccco2)c2ccco2)c1>COc1nc(Nc2cc(C(F)(F)F)ccc2F)ncc1Br

Participants

7

Conditions

Temperature
90 °C

Procedure

To a microwave vial was added a mixture of 5-bromo-4-methoxypyrimidin-2-amine (0.513 g, 2.51 mmol), diacetoxypalladium (0.055 g, 0.245 mmol), tri(furan-2-yl)phosphine (0.126 g, 0.54 mmol), 1-fluoro-2-iodo-4-(trifluoromethyl)benzene (0.98 g, 3.38 mmol) and toluene (17 mL) under inert atmosphere. The reaction mixture was sealed and heated at 90 °C under 15h. The LCMS indicated no reaction ??? The sample discarded.

Sources & evidence

ORD record
ord-f903bfa68e6e46fb8291b98645969acd
Source dataset
750 AstraZeneca ELN dataset
Original link
View source

Linked notes

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