Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | 3-Fluorobenzoyl chloride | HCID 74376 | — |
| Reactant | Ethyl 2-[(3-nitropyridin-2-YL)amino]acetate | HCID 14062544 | — |
| Reactant | Ethyl 2-(3-aminopyridin-2-ylamino)acetate | HCID 14390203 | — |
| Catalyst | Palladium | HCID 23938 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | HCID 14390498 | HCID 14390498 | 6.6% |
Reaction Steps
Under a nitrogen atmosphere, 3-fluorobenzoyl chloride (12.9 g, 0.0816 mole) was added dropwise to a stirred and chilled (10°-15° C.) mixture of N-(3-amino-2-pyridinyl)glycine ethyl ester (0.0816 mole) [freshly prepared by the hydrogenation of a solution of N-(3-nitro-2-pyridinyl)glycine ethyl ester in tetrahydrofuran over 5% palladium on carbon at room temperature], triethylamine (8.3 g, 0.0816 mole), anhydrous tetrahydrofuran (200 ml), and powdered molecular sieves. The reaction mixture was stirred at room temperature for 1 hour and was filtered. The filtrate was concentrated in vacuo and the residual solid triturated in isopropyl ether-isopropyl alcohol, giving 24.2 g (94%). Recrystallization of a 2.0-g sample gave 1.72 g of a white powder, mp 134°-135° C.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US04824951 |
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| Source dataset | uspto-grants-1989_04 |
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| ORD ID | ord-4e06be272b9743438ac7af9886ebad92 |
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| Source note | uspto-grants-1989_04 |
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