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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 2095095Erstellt: 26. Oktober 2026

Methylamine → Tadalafil

https://huagongshe.com/reaction/2095095

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktMethylamineHCID 6329—
Edukt(1S,3S)-1-(1,3-Benzodioxol-5-yl)-2-(2-chloroacetyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic Acid Methyl EsterHCID 68502869—
LösungsmittelMethanolHCID 887—
ProduktTadalafilHCID 110635—

Reaktionsbedingungen

Temperatur52.5 °C

Reaktionsschritte

Cis-1 -benzo [1,3 ]dioxol-5 -yl-2-(2-chloro-acetyl)-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid methyl ester (30 g) was taken in methanol (450 ml). The resultant mixture was heated to 35-40° C. and aqueous methyl amine (27 ml; 40%) was added. The reaction mixture was stirred at 50-55° C. for 5 hours and then cooled to 10-15° C. with continuous stirring for 0.5 hours. The solid so obtained was filtered and dried to afford (6R,12aR) 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino [1′,2′:1,6] pyrido[3,4-b]indole-1,4-dione.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08445698B2
Quelldatensatzuspto-grants-2013_05
ORD IDord-94c1d194673c4f0caf639c2655e57a4d
Quellennotizuspto-grants-2013_05