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Buchwald–Hartwig amination, record ord-8cfc6888cfb048a3bbd7a788345f4499

One recorded run of this reaction. Below is what the source recorded, and nothing added to it.

verified record62% yield recordedNot balanced as writtenFrom experimental reaction archive

Reactants and products as the record gives them. Reagents, catalysts and solvents are listed below rather than drawn.

Open this record in the Reaction LabThe atom map, the animation and the records that run the same transformation.

What was in the flask

RoleSpeciesFormulaYield
Reactant7-Bromo-1-benzofuranC₈H₅BrO
Reactant1-PhenethylpiperazineC₁₂H₁₈N₂
Reagentsodium 2-methylpropan-2-olateC₄H₉NaO
CatalystBinap, (A+-)-C₄₄H₃₂P₂
CatalystBis(dibenzylideneacetone)palladiumC₅₁H₄₂O₃Pd₂
SolventTolueneC₇H₈
Product1-Benzofuran-7-yl-4-phenethyl-piperazine; hydrochlorideC₂₀H₂₂N₂O62.12%

The equation does not balance as written. That is usual for an experimental record: the source listed what it put in and what it measured, not a stoichiometric equation.

Conditions

Temperature
110 °C

Only the dimensions the source stated are listed. Anything absent here was not recorded, and it is not inferred from what the class usually needs.

Yield

  • 62% of 1-Benzofuran-7-yl-4-phenethyl-piperazine; hydrochloride.

Procedure

Copied from the source record, unedited

A dried Radley tube was charged with rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (6.32 mg, 10.15 µmol), Tris(dibenzylideneacetone)dipalladium(0) (4.65 mg, 5.08 µmol) and Sodium tert- butoxide (34.1 mg, 0.36 mmol). Argon atmosphere was introduced and toluene (3ml) was added followed by 7-bromobenzofuran (50mg, 0.25 mmol) and 1-phenethylpiperazine (48.3 mg, 0.25 mmol). The reaction mixture was heated at reflux over night. 2010-03-25 The reaction mixture was filtered, concentrated and purified by flash chromatography (Isolute Si 10g, heptane: ethyl acetate; 4:1) to give 1-(benzofuran-7-yl)-4-phenethylpiperazine (48.3 mg, 62.1 %)

The source

This record comes from experimental reaction archive (ord-8cfc6888cfb048a3bbd7a788345f4499). Open the source and check it against what is on this page.

  • experimental reaction archive record ord-8cfc6888cfb048a3bbd7a788345f4499 from dataset "750 AstraZeneca ELN dataset" (url: https://chemrxiv.org/engage/chemrxiv/article-details/60c9e3f37792a23bfdb2d471). No atom mapping is provided by the source.

    experimental record · quality medium · source

experimental reaction record.

How to read this record

This is one experiment, not a rule. It says that on one occasion these species were combined under these conditions and this came out. It does not say the reaction will give the same result on your substrate, and nothing on the page has been generalised into a claim that it would.

The pathway is a separate question, kept on separate pages. A mechanism here is the canonical arrow pushing for a class, run on real structures and labelled rule-derived. It is not evidence, and this record is not a mechanism.