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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 80560Erstellt: 25. Oktober 2026

Potassium Carbonate → 1-(2-Chloro-3,6-difluorobenzyl)-8-methyl-7-[3-(morpholin-4-yl)phenyl]-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine

https://huagongshe.com/reaction/80560

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktPotassium CarbonateHCID 11430—
Edukt4-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)morpholineHCID 4192663—
Edukt7-Bromo-1-(2-chloro-3,6-difluorobenzyl)-8-methyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazineHCID 67007063—
KatalysatorHCID 178418476HCID 178418476—
LösungsmittelN,N-Dimethylformamide--water (1/1)HCID 21962138—
Produkt1-(2-Chloro-3,6-difluorobenzyl)-8-methyl-7-[3-(morpholin-4-yl)phenyl]-1,2,3,4-tetrahydropyrido[2,3-b]pyrazineHCID 6700826940%

Reaktionsschritte

To a solution of 7-bromo-1-(2-chloro-3,6-difluorobenzyl)-8-methyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (0.048 g, 0.124 mmol) and 3-morpholinophenylboronic acid pinacol ester (0.035 g, 0.124 mmol) in DMF-H2O (9:1, 2 mL) was added PdCl2(PPh3)2 (0.0087 g, 0.0124 mmol) and K2CO3 (0.043 mg, 0.31 mmol). The resulting solution was subjected to microwave irradiation at 125° C. for 20 min. The solvent was filtered using a PTFE frit and then directly purified by prep HPLC using a gradient mixture of ACN—H2O— 0.1% TFA to yield the desired product (0.023 g 40%).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08846664B2
Quelldatensatzuspto-grants-2014_09
ORD IDord-6e4ab137b7c647629183be7e639441a0
Quellennotizuspto-grants-2014_09