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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1244096Generated: October 31, 2026

Acetic Acid → 4-Hydroxy-6-oxo-3-{2'-[({2-[4-(trifluoromethyl)phenyl]ethyl}amino)methyl]-1,1'-biphenyl-4-yl}-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile

https://huagongshe.com/reaction/1244096

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAcetic AcidHCID 176—
ReactantCyano-borohydrideHCID 498716—
Reactant2-[4-(Trifluoromethyl)phenyl]ethan-1-amineHCID 1988106—
Reactant3-(2'-Formyl-1,1'-biphenyl-4-yl)-4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrileHCID 54689942—
SolventMethanolHCID 887—
SolventDichloromethaneHCID 6344—
Product4-Hydroxy-6-oxo-3-{2'-[({2-[4-(trifluoromethyl)phenyl]ethyl}amino)methyl]-1,1'-biphenyl-4-yl}-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrileHCID 54678056—

Reaction Steps

To a solution of 3-(2′-formyl-1,1′-biphenyl-4-yl)-4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile (0.025 g, 0.067 mmol) in MeOH (1 mL) and dichloromethane (1 mL, with 2% v/v acetic acid) was added 2-(4-trifluoromethyl phenyl)ethyl amine (0.025 g, 0.13 mmol) and shaken at room temperature for 10 min. MP-cyanoborohydride (0.09 g, 0.2 mmol) was then added to the reaction mixture and shaken at room temperature for 24 h. The reaction was filtered, concentrated and purified by RP-HPLC to give the title compound. MS (ESI) m/e 546 (M+H)+; 1H NMR (500 MHz, DMSO-d6): δ ppm 11.11 (br s, 1H), 8.97 (br s, 2H), 7.66–7.70 (m, 3H), 7.58 (d, 2H), 7.50–7.54 (m, 2H), 7.46 (d, 2H), 7.37–7.40 (m, 1H), 7.30 (d, 2H), 6.76 (s, 1H), 4.24 (s, 2H), 3.17 (br s, 2H), 2.95 (t, 2H).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07119205B2
Source datasetuspto-grants-2006_10
ORD IDord-a59af4cc29ae435eb4e6b114765ccd74
Source noteuspto-grants-2006_10