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Buchwald–Hartwig amination, record ord-0eb7fc5c164b43bc9a05a46e98a37b12

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

verified record15% 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
ReactantIodobenzeneC₆H₅I
Reactant4-Methoxy-2-aminobenzothiazoleC₈H₈N₂OS
Reagentsodium 2-methylpropan-2-olateC₄H₉NaO
Catalyst1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)C₃₉H₃₂OP₂
CatalystBis(dibenzylideneacetone)palladiumC₅₁H₄₂O₃Pd₂
SolventTolueneC₇H₈
Product4-methoxy-N-phenylbenzo[d]thiazol-2-amineC₁₄H₁₂N₂OS15.22%

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
90 °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

  • 15% of 4-methoxy-N-phenylbenzo[d]thiazol-2-amine.

Procedure

Copied from the source record, unedited

4-methoxybenzo[d]thiazol-2-amine (0.216 g, 1.20 mmol), iodobenzene (0.112 mL, 1.00 mmol), XANTPHOS (0.058 g, 0.10 mmol), Pd2(dba)3 (0.027 g, 0.03 mmol) and SODIUM TERT-BUTOXIDE (0.192 g, 2.00 mmol) placed in a sealed reaction via under an atmosphere of nitrogen and heated at 90ºC for 1 hour. LC/MS indicated mainly product, little SM. Cooled, diluted DCM and washed with water and brine. Org phase dried/MgSO4, filtered and evaporated. The crude product was purified by flash silica chromatography, eluting with dichloromethane. Pure fractions were evaporated to dryness to afford 4-methoxy-N- phenylbenzo[d]thiazol-2-amine (0.039 g, 15.22 %) as an colorless solid. EN01327-44-1 (0.039 g, 0.15 mmol, 15.22 %) Not sure why yield so low, crude lc/ms looked fine. Reaction left for several days before

The source

This record comes from experimental reaction archive (ord-0eb7fc5c164b43bc9a05a46e98a37b12). Open the source and check it against what is on this page.

  • experimental reaction archive record ord-0eb7fc5c164b43bc9a05a46e98a37b12 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.