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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 400838Erstellt: 25. Oktober 2026

1,8-Diazabicyclo(5.4.0)undec-7-ene → 5-tert-Butyl-3-(2-chloro-benzyl)-7-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine

https://huagongshe.com/reaction/400838

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
Edukt1,8-Diazabicyclo(5.4.0)undec-7-eneHCID 81184—
Edukt1,3-PropanesultamHCID 642157—
Edukt5-tert-butyl-7-chloro-3-(2-chlorobenzyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidineHCID 86683284—
LösungsmittelDimethylformamideHCID 6228—
Produkt5-tert-Butyl-3-(2-chloro-benzyl)-7-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidineHCID 8668329016%

Reaktionsschritte

A mixture of 5-tert-butyl-7-chloro-3-(2-chlorobenzyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine (15.9 mg, 47.2 μmol), 1,1-dioxo-isothiazolidine (11.4 mg, 94.4 μmol) and DBU (14.2 μL, 94.4 μmol) in DMF (250 μL) was stirred at the room temperature overnight. The reaction mixture was directly purified by preparative HPLC (column: Gemini Sum C18 110A 75×30 mm. mobile phase: water (0.05% Et3N): acetonitrile 75:25% to 5:95%. WL: 230 nm Flow: 30 mL/min.) to afford the title compound as white solid (3.10 mg, 16%). MS (m/e): 387.3 (MH+).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08741906B2
Quelldatensatzuspto-grants-2014_06
ORD IDord-80588c1206c5471db8ded5e80daec0fa
Quellennotizuspto-grants-2014_06