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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 421932Erstellt: 26. Oktober 2026

1,2-Dichloroethane → Tert-butyl{2-[[(7r)-11-({[(3-chloropropyl)sulfonyl]amino}carbonyl)-14-cyclohexyl-7,8-dihydro-6h-indolo[1,2-e][1,5]benzoxazocin-7-yl](methyl)amino]ethyl}carbamate

https://huagongshe.com/reaction/421932

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
Edukt1,2-DichloroethaneHCID 11—
Edukt3-Chloropropane-1-sulfonamideHCID 13614818—
Edukt(7R)-7-[{2-[(tert-butoxycarbonyl)amino]ethyl}(methyl)amino]-14-cyclohexyl-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acidHCID 66674687—
Katalysator4-(Dimethylamino)pyridineHCID 14284—
LösungsmittelDichloromethaneHCID 6344—
ProduktTert-butyl{2-[[(7r)-11-({[(3-chloropropyl)sulfonyl]amino}carbonyl)-14-cyclohexyl-7,8-dihydro-6h-indolo[1,2-e][1,5]benzoxazocin-7-yl](methyl)amino]ethyl}carbamateHCID 86622849—

Reaktionsbedingungen

Temperatur40 °C

Reaktionsschritte

3-chloropropane-1-sulfonamide (1.8 eq), DMAP (2.9 eq) and EDC (1.8 eq), were added to a solution of (7R)-7-[{2-[(tert-butoxycarbonyl)amino]ethyl}(methyl)amino]-14-cyclohexyl-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (prepared as described in Example 1, Step 7) (0.025 M) in DCM. The reaction was stirred under N2 at 40° C. for 2 h, before being allowed to cool. Volatiles were removed in vacuo to leave the crude product as a yellow gum which could be taken on without further purification. (ES+) m/z 687 (M+H)+; 689 (M+H)+

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08101595B2
Quelldatensatzuspto-grants-2012_01
ORD IDord-dd02d376464e4968b8a6dd21f3bd5c29
Quellennotizuspto-grants-2012_01