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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 540995Erstellt: 25. Oktober 2026

Dichloromethane → Tadalafil Impurity 11

https://huagongshe.com/reaction/540995

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktDichloromethaneHCID 6344—
EduktPiperonalHCID 8438—
Eduktmethyl (2R)-2-amino-3-(1H-indol-3-yl)propanoate hydrochlorideHCID 11448200—
LösungsmittelSulfolaneHCID 31347—
ProduktTadalafil Impurity 11HCID 44250481—

Reaktionsschritte

D-tryptophan methyl ester hydrochloride of Step 1 (100 g) and piperonal (65 g) were suspended in sulfolane (500 mL) at 25° C. to 30° C. The reaction mixture was heated to 80° C. to 85° C., stirred for 14 hours, and then cooled to 25° C. to 30° C. To the cooled mixture, dichloromethane (500 mL) was added and the resultant mixture was stirred continuously for 1 hour. The solid obtained was filtered, washed with dichloromethane (500 mL), and dried in air at 40° C. to 45° C. to afford cis 1-benzo[1,3]dioxol-5-yl-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid methyl ester hydrochloride.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08871932B2
Quelldatensatzuspto-grants-2014_10
ORD IDord-8b682bd17854417093b72289a6c1f573
Quellennotizuspto-grants-2014_10