Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | Ethanimidic acid, ethyl ester, hydrochloride (1:1) | HCID 2724290 | — |
| Reactant | Bis-(3-methyl-pyridin-2-ylmethyl)-piperidin-4-yl-amine | HCID 58996965 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | HCID 58996981 | HCID 58996981 | 34.1% |
Reaction Steps
To a solution of COMPOUND 249 (0.1054 g, 0.34 mmol) in MeOH (4 mL) was added Et3N (0.1 mL, 0.68 mmol) and ethyl acetimidate hydrochloride (0.0549 g, 0.41 mmol), and stirred at room temperature for 24 hours then concentrated. Saturated NaHCO3 (15 mL) was added and extracted with CH2Cl2 (2×40 mL). Purification of the crude material by column chromatography on silica gel (15:1:1 CH2Cl2-MeOH—NH4OH) followed by radial chromatography on silica gel (50:3:2 CH2Cl2-MeOH—NH4OH) provided 0.0408 g (34%) of COMPOUND 338 as a white solid. 1H NMR (CDCl3) δ 1.60-1.72 (m, 2H), 1.90-1.95 (m, 2H), 2.09 (s, 6H), 2.12 (s, 3H), 2.47-2.68 (m, 4H), 3.82 (s, 4H), 4.17 (d, 2H, J=12.3 Hz), 7.06-7.10 (m, 2H), 7.37 (d, 2H, J=7.2 Hz), 8.34 (d, 2H, J=4.5 Hz). 13C NMR (CDCl3) δ 18.39, 23.92, 27.33, 45.64, 55.06, 57.89, 122.77, 133.81, 138.40, 146.29, 157.63, 164.64. ES-MS m/z 352.5 (M+H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07291631B2 |
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| Source dataset | uspto-grants-2007_11 |
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| ORD ID | ord-78afb9d8ea55419d9edad26c78bcc5ab |
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| Source note | uspto-grants-2007_11 |
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