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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 882065Generated: October 31, 2026

Hydrochloric Acid → 1-(1,2,3,4-Tetrahydropyrazino[1,2-a]benzimidazol-8-yl)-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-one

https://huagongshe.com/reaction/882065

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
Reactanttert-Butyl 8-(2-oxo-4-(4-(trifluoromethyl)phenyl)pyridin-1(2H)-yl)-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylateHCID 68056088—
Product1-(1,2,3,4-Tetrahydropyrazino[1,2-a]benzimidazol-8-yl)-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-oneHCID 5752476053%

Reaction Steps

tert-Butyl 8-(2-oxo-4-(4-(trifluoromethyl)phenyl)pyridin-1(2H)-yl)-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylate (15 mg, 0.023 mmol) was deprotected and converted to the hydrochloride according to Example 18 (step h) to provide the title compound (5 mg, 38%) as an orange solid: 1H NMR (500 MHz, DMSO-d6) δ 9.71 (s, 2H), 8.01 (d, J=8.3 Hz, 2H), 7.88 (d, J=8.3 Hz, 2H), 7.82 (d, J=7.8 Hz, 1H), 7.75 (m, 2H), 7.37 (d, J=8.4 Hz, 1H), 6.88 (s, 1H), 7.73 (d, J=7.5 Hz, 1H), 4.67 (s, 2H), 4.47-4.41 (m, 2H), 3.83-3.77 (m, 2H); ESI MS m/z 411 [M+H]+; HPLC (Method B) 91.3% (AUC), tR=12.8 min.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08993765B2
Source datasetuspto-grants-2015_03
ORD IDord-78675af589c3484c90883749fa7f6e3d
Source noteuspto-grants-2015_03