Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Dimethyl Sulfide | HCID 1068 | — |
| Reactant | 2-(2-Bromo-benzyloxy)-5-chloro-benzonitrile | HCID 59772382 | — |
| Solvent | 1,2-Dichloroethane | HCID 11 | — |
| Product | HCID 59772401 | HCID 59772401 | 60% |
Reaction Steps
To a stirred solution of 2-(2-Bromo-benzyloxy)-5-chloro-benzonitrile Example 348A (1.52 g, 4.71 mmol) in DCE (50 mL) under argon was added BH3 DMS (30.0 mL, 18.8 mmol). The reaction mixture was heated at 65° C. for 14 h and then cooled to room temperature. The mixture was quenched with 1N HCl solution slowly (25 mL). This solution was then mixed with 1N NaOH solution (30 mL), and extracted with EtOAc (3×80 mL). The combined EtOAc extracts were washed with saturated NaHCO3 solution (1×40 mL) and brine (1×40 mL). The organic layer was dried (MgSO4), filtered and concentrated in vacuo to give 0.92 g (60%) of crude 2-(2-Bromo-benzyloxy)-5-chloro-benzylamine Example 348B which was used as is without further purification. HPLC Rt=2.87 min (YMC S5 ODS column 4.6×50 mm, 10-90% aqueous methanol over 4 minutes containing 0.2% phosphoric acid, 4 mL/min, monitoring at 220 nm) LC/MS: M+H=326
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07417040B2 |
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| Source dataset | uspto-grants-2008_08 |
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| ORD ID | ord-de831421b86341ccae5bd017d3ffeba7 |
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| Source note | uspto-grants-2008_08 |
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