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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 1162787Erstellt: 24. Oktober 2026

Formic Acid → 2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide

https://huagongshe.com/de/reaction/1162787

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktFormic AcidHCID 284—
EduktMethylamineHCID 6329—
Edukt2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonateHCID 59520461—
LösungsmittelDimethylformamideHCID 6228—
Produkt2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamideHCID 5952046613,1%

Reaktionsbedingungen

Temperatur120 °C

Reaktionsschritte

The 2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonate (30 mg, 0.061 mmol) was dissolved in DMF (1 mL) and methylamine (2 M in THF, 1 mL, 2 mmol) added. The reaction mixture was heated at 120° C. for 5 min in the microwave. The THF was removed in vacuo and the reaction mixture filtered and purified by preparative reverse phase HPLC to give the formic acid salt of the desired product (3.6 mg, 0.008 mmol, 12%).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS07820707B2
Quelldatensatzuspto-grants-2010_10
ORD IDord-4fcfae59353649e49cdea4ee85fd3982
Quellennotizuspto-grants-2010_10