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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1697982Generated: October 30, 2026

Phosgene → HCID 86640110, compound

https://huagongshe.com/reaction/1697982

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPhosgeneHCID 6371—
ReactantTriethylamineHCID 8471—
Reactant2-FluoroethylamineHCID 9996—
Reactant1,4-DioxaneHCID 31275—
Reactant(S)-4-(4-(3-methylmorpholino)-7-(pyrimidin-2-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)anilineHCID 67176513—
SolventTolueneHCID 1140—
ProductHCID 86640110HCID 86640110—

Reaction Conditions

Temperature50 °C

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

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08163763B2
Source datasetuspto-grants-2012_04
ORD IDord-96060be1474b4e3a851d8c8ef3b42429
Source noteuspto-grants-2012_04