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Buchwald–Hartwig amination, record ord-11b483655b194597ac2e93597b6914d4

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

verified record28% 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
Reactant3-BromoanisoleC₇H₇BrO
Reactant4-CyanopiperidineC₆H₁₀N₂
Reagentlithium bis(trimethylsilyl)azanideC₆H₁₈LiNSi₂
Catalyst2,8,9-Triisobutyl-2,5,8,9-tetraaza-1-phosphabicyclo(3.3.3)undecaneC₁₈H₃₉N₄P
CatalystPalladium (II) acetateC₄H₈O₄Pd
SolventTolueneC₇H₈
Product1-(3-Methoxyphenyl)piperidine-4-carbonitrileC₁₃H₁₆N₂O28.45%

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
100 °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

  • 28% of 1-(3-Methoxyphenyl)piperidine-4-carbonitrile.

Procedure

Copied from the source record, unedited

Reaction carried out by , work up and purification on this page. piperidine-4-carbonitrile (7.07 g, 64.16 mmol); 1-bromo-3-methoxybenzene (6.77 mL, 53.47 mmol) and diacetoxypalladium (2.401 g, 10.69 mmol) were thoroughly placed under an inert atmoshere. To this was added 2,8,9-triisobutyl-2,5,8,9-tetraaza-1-phosphabicyclo[3.3.3]undecane (0.732 g, 2.14 mmol); LITHIUM BIS(TRIMETHYLSILYL)AMIDE (123 mL, 122.97 mmol) and toluene (20 mL). The resultant mixture was stirred overnight at 100 °C (suspect that it did not need overnight. The reaction mixture was poured onto DCM (200 mL), the mixture was filtered through celite and evaporated to afford a black residue. This was suspended in EtOAc (200 mL) and water (20 mL) and filtered through a pad of silica, washing through with EtOAc (300 mL) and w

The source

This record comes from experimental reaction archive (ord-11b483655b194597ac2e93597b6914d4). Open the source and check it against what is on this page.

  • experimental reaction archive record ord-11b483655b194597ac2e93597b6914d4 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.