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Sodium Carbonate → HCID 101656270, Verbindung

HRID 333699
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Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 333699
ClC1C=C(C=CC=1)C(OO)=[O:6].[CH3:12][CH2:13][C:14]1[CH2:31][N:29]2[CH2:30][C@H:16]([CH2:17][C@:18]([C:65]([O:67][CH3:68])=[O:66])([C:32]3[CH:33]=[C:34]4[C@:42]56[C@@H:46]7[C@:47]([CH2:62][CH3:63])([C@@H:51]([O:58][C:59]([CH3:61])=[O:60])[C@:52]([OH:57])([C:53]([O:55][CH3:56])=[O:54])[C@@H:41]5[N:40]([CH3:64])[C:35]4=[CH:36][C:37]=3[O:38][CH3:39])[CH:48]=[CH:49][CH2:50][N:45]7[CH2:44][CH2:43]6)[C:19]3[NH:27][C:26]4[CH:25]=[CH:24][CH:23]=[CH:22][C:21]=4[C:20]=3[CH2:28]2)[CH:15]=1.C(=O)([O-])[O-].[Na+].[Na+]>C(Cl)(Cl)Cl>[CH3:12][CH2:13][C:14]1[CH2:31][N:29]2[CH2:30][C@@H:16]([CH2:17][C@:18]([C:65]([O:67][CH3:68])=[O:66])([C:32]3[CH:33]=[C:34]4[C@@:42]56[C@@H:41]([N:40]([CH3:64])[C:35]4=[CH:36][C:37]=3[O:38][CH3:39])[C@@:52]([OH:57])([C:53]([O:55][CH3:56])=[O:54])[C@H:51]([O:58][C:59]([CH3:61])=[O:60])[C@:47]3([CH2:62][CH3:63])[CH:48]=[CH:49][CH2:50][N:45]([C@H:46]53)[CH2:44][CH2:43]6)[C:19]3[NH+:27]([O-:6])[C:26]4[C:21](=[CH:22][CH:23]=[CH:24][CH:25]=4)[C:20]=3[CH2:28]2)[CH:15]=1
KomponentenVersuchsvorschriftAufarbeitungQuellen und NachweiseNotizen zur Reaktion

Komponenten

5

Edukt 3

HCID 10340Sodium CarbonateHCID 70297m-Chloroperbenzoic acidHCID 5311497Vinorelbine

Produkt 1

HCID 101656270HCID 101656270, VerbindungAusbeute 83 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6212ChloroformLösungsmittel2×

Versuchsvorschrift

Vinorelbine N′b-oxide was synthesized using essentially the same procedure used to prepare vinblastine N′b-oxide. m-Chloroperoxybenzoic acid (45 mg, 0.26 mmol) in CHCl3 (2.5 mL) was added at 0° to a stirred solution of purified vinorelbine (150 mg, 0.20 mmol) in CHCl3 (4.5 mL) under nitrogen. After 15 min, the mixture was poured into an aqueous sodium carbonate (27 mL, 40 g/L) and was extracted by CHCl3 (20 mL). After drying over sodium sulfate and filtration, the CHCl3 extract was evaporated under reduced pressure affording crude vinorelbine N-oxide (125 mg, 83%). Thin-layer chromatography (silica; 9:1 CHCl3/MeOH) indicated the presence of a small amount of starting vinorelbine (vinorelbine Rf=0.37, vinorelbine N′b-oxide Rf=0.18). Radial chromatography on silica gel (eluent, 9:1 CHCl3/MeOH) gave vinorelbine N′b-oxide as an off-white solid (100 mg; 75%). The sample was dissolved in ethyl acetate/hexanes and then the open flask was placed in a sealed container containing an open flask of hexanes. As the hexanes diffused slowly into the vinorelbine N′b-oxide solution, vinorelbine N′b-oxide precipitated out as an off-white powder (80 mg; 53%). The 300 MHz 1HNMR spectrum was consistent with the assigned structure. The configuration of the N′b-oxide oxygen atom is assigned the same stereochemistry as that found in vinblastine N-oxide by x-ray crystallography.

Aufarbeitung

  1. extractionwas extracted by CHCl3 (20 mL)
  2. dry with materialAfter drying over sodium sulfate and filtration
  3. extractionthe CHCl3 extract
  4. customwas evaporated under reduced pressure

Quellen und Nachweise

ORD-Eintrag
ord-9eee79bb7ea246f4836bd07718942240
Quelldatensatz
uspto-grants-2014_11
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US08883775B2

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