Skip to the content
Browse the library

Buchwald–Hartwig amination, record ord-a9eb8bf838c248b3ad5908714b48274f

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

verified record0% 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
Reactant5-Chloro-2-iodoanisoleC₇H₆ClIO
Reactant1-MethylpiperazineC₅H₁₂N₂
Reagentsodium 2-methylpropan-2-olateC₄H₉NaO
CatalystBinap, (A+-)-C₄₄H₃₂P₂
CatalystPalladium (II) acetateC₄H₈O₄Pd
SolventTolueneC₇H₈
Product1-(4-Chloro-2-methoxyphenyl)-4-methylpiperazineC₁₂H₁₇ClN₂O0%

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
80 °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

  • 0% of 1-(4-Chloro-2-methoxyphenyl)-4-methylpiperazine.

Procedure

Copied from the source record, unedited

1-methylpiperazine (0.021 mL, 0.19 mmol) was added to 4-chloro-1-iodo-2-methoxybenzene (50 mg, 0.19 mmol) and sodium 2-methylpropan-2-olate (35.8 mg, 0.37 mmol) in toluene (0.650 mL) and the solution degassed. rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (11.60 mg, 0.02 mmol) and Palladium II acetate (4.18 mg, 0.02 mmol) were added to the resulting mixture and the vial stirred at 80 °C for 17 hours. LCMS revelead product peak, but not great. Product not isolated.

The source

This record comes from experimental reaction archive (ord-a9eb8bf838c248b3ad5908714b48274f). Open the source and check it against what is on this page.

  • experimental reaction archive record ord-a9eb8bf838c248b3ad5908714b48274f 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.