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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 1262150Erstellt: 26. Oktober 2026

2-(5-Amino-1,3-dihydro-2H-isoindol-2-yl)acetamide → 2-{5-[7-(2-Methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-1,3-dihydro-isoindol-2-yl}-acetamide

https://huagongshe.com/reaction/1262150

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
Edukt2-(5-Amino-1,3-dihydro-2H-isoindol-2-yl)acetamideHCID 57416055—
EduktTrifluoro-methanesulfonic acid 7-(2-methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl esterHCID 86661678—
LösungsmittelPropylene glycol methyl etherHCID 3032390—
Produkt2-{5-[7-(2-Methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-ylamino]-1,3-dihydro-isoindol-2-yl}-acetamideHCID 66712188—

Reaktionsschritte

Trifluoro-methanesulfonic acid 7-(2-methoxy-phenyl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl ester (0.111 g, 0.298 mmol) and 2-(5-Amino-1,3-dihydro-isoindol-2-yl)-acetamide (0.077 g, 0.40 mmol) were reacted in an analogous manner to Example 908D at 50° C. for 16 h in methoxypropanol. Pale yellow solid was filtered off, washed with water. Found to be pure product (35 mg, 28%). LCMS=414.9 (M+H), HPLC rt=2.256 min, purity=99%. 1H NMR (400 MHz, (D3C)2SO, δ, ppm): 9.40 (s, 1H), 8.95 (s, 1H), 7.78 (d, J=7.4 Hz, 1H), 7.75 (s, 1H), 7.47 (dd, J=7.6 Hz, 1H), 7.39 (d, J=8.6 Hz, 1H), 7.32 (s, 1H), 7.21 (d, J=8.6 Hz, 1H), 7.13-7.05 (m, 3H), 6.94 (d, J=4.6 Hz, 1H), 6.90 (d, J=4.6 Hz, 1H), 3.89 (s, 4H0, 3.78 (s, 3H), 3.27 (s, 2H).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08471005B2
Quelldatensatzuspto-grants-2013_06
ORD IDord-34a60d3ef9c3481db657413df6df6d9e
Quellennotizuspto-grants-2013_06