1,2-Dichloroethane → 2-Deoxyglucose

HRID 1353987

Reaktionsgleichung

Reaktionsgleichung von HRID 1353987
[OH-].[Na+].C1C(=O)N(O)C(=O)C1S([O-])(=O)=O.[Na+].C(Cl)CCl.Cl.[OH:21][CH:22]1[O:30][C@H:29]([CH2:31][OH:32])[C@@H:27]([OH:28])[C@H:25]([OH:26])[C@H:23]1N>O>[O:21]=[CH:22][CH2:23][C@H:25]([C@@H:27]([C@@H:29]([CH2:31][OH:32])[OH:30])[OH:28])[OH:26]

Komponenten

6

Edukt 4

HCID 111,2-DichloroethaneHCID 14798Sodium HydroxideHCID 2723635(3R,4R,5S,6R)-3-amino-6-(hydroxymethyl)oxane-2,4,5-triol hydrochlorideHCID 3520574n-hydroxysulfosuccinimide sodium salt

Produkt 1

HCID 1082232-Deoxyglucose

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 962WaterLösungsmittel

Versuchsvorschrift

Sodium hydroxide (1N, 1 ml) was added to a stirred solution of EC (110 mg, 0.41 mmol) in water (5 ml). To this colorless solution, sulfo-NHS (241.6 mg, 1.12 mmol) and EDC (218.8 mg, 1.15 mmol) were added. D-Glucosamine hydrochloride salt (356.8 mg, 1.65 mmol) was then added. The mixture was stirred at room temperature for 24 hours. The mixture was dialyzed for 48 hours using Spectra/POR molecular porous membrane with cut-off at 500 (Spectrum Medical Industries Inc., Houston, Tex,). After dialysis, the product was frozen dried using lyophilizer (Labconco, Kansas City, Mo.). The product in the salt form weighed 568.8 mg. The synthetic scheme is shown in FIG. 59. The structure was confirmed by mass spectrometry (FIG. 60) and proton NMR (FIGS. 61 and 62). Radiochemical purity of 99mTc-EC-DG was 100% as determined by radio-TLC (FIG. 63) and HPLC (FIGS. 64 and 65) analysis.

Aufarbeitung

  1. customThe mixture was dialyzed for 48 hours
  2. customAfter dialysis
  3. temperaturethe product was frozen
  4. customdried

Quellen und Nachweise

ORD-Eintrag
ord-8150cb28e52e46609954cb80d3fdf66d
Quelldatensatz
uspto-grants-2007_05
Patentnummer
US07223380B2

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