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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1772072Generated: November 2, 2026

Hydrochloric Acid → 4-tert-Butyl-2-((2-methyl-3-(4-methyl-6-(4-(morpholine-4-carbonyl)-phenylamino)-5-oxo-4,5-dihydropyrazin-2-yl)phenylamino)methyl)benzoic Acid

https://huagongshe.com/reaction/1772072

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
ReactantLithium HydroxideHCID 3939—
ReactantEthyl 4-tert-Butyl-2-((2-methyl-3-(4-methyl-6-(4-(morpholine-4-carbonyl)phenyl amino)-5-oxo-4,5-dihydropyrazin-2yl)phenylamino)methyl)benzoateHCID 66610366—
SolventEthanolHCID 702—
SolventWaterHCID 962—
SolventTetrahydrofuranHCID 8028—
Product4-tert-Butyl-2-((2-methyl-3-(4-methyl-6-(4-(morpholine-4-carbonyl)-phenylamino)-5-oxo-4,5-dihydropyrazin-2-yl)phenylamino)methyl)benzoic AcidHCID 66610147—

Reaction Conditions

Temperature60 °C

Reaction Steps

To 25 mL round bottom flask charged with ester 101h (100 mg, 0.16 mmol) and LiOH (20 mg, 0.47 mmol) in THF (2 mL), EtOH (2 mL) and H2O (2 mL). After the mixture was stirred at 60° C. for 16 h, the pH was adjusted to 7 with aqueous 1M HCl. The aqueous phase was extracted with EtOAc (2×10 mL), and the combined organic extracts were washed with brine (10 mL), dried with Na2SO4 and concentrated. The crude 101i (97 mg, 99%) was used without further purification.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09249123B2
Source datasetuspto-grants-2016_02
ORD IDord-2c2685f96f5c4cd980be8842fd2f4686
Source noteuspto-grants-2016_02