Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Phosgene | HCID 6371 | — |
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | 2-Fluoroethylamine | HCID 9996 | — |
| Reactant | 1,4-Dioxane | HCID 31275 | — |
| Reactant | (S)-4-(4-(3-methylmorpholino)-7-(pyrimidin-2-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)aniline | HCID 67176513 | — |
| Solvent | Toluene | HCID 1140 | — |
| Product | HCID 86640110 | HCID 86640110 | — |
Reaction Steps
(S)-4-(4-(3-methylmorpholino)-7-(pyrimidin-2-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)aniline (0.0501 g, 0.000124 mol) in dry 1,4-Dioxane (2.00 mL, 0.0256 mol) was added Triethylamine (0.0190 mL, 0.000136 mol) followed by 20% Phosgene in toluene (1:4, Phosgene:Toluene, 0.080 mL). The reaction mixture was heated at 50° C. for 1 hour. The reaction mixture was cooled to room temperature and then added 2-fluoroethanamine (0.0534 g, 0.000762 mol) followed by Triethylamine (0.1140 mL, 0.0008179 mol). The reaction mixture was stirred for 3 days. The reaction mixture was concentrated and purified by HPLC. LC/MS-m/z+493.2 (M+H)+
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08163763B2 |
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| Source dataset | uspto-grants-2012_04 |
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| ORD ID | ord-96060be1474b4e3a851d8c8ef3b42429 |
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| Source note | uspto-grants-2012_04 |
|---|