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Acetic Acid → HCID 60207424, Verbindung

HRID 1192204
Notizen
Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 1192204
[Cl:1][C:2]1[CH:3]=[N:4][CH:5]=[C:6]([Cl:25])[C:7]=1[S:8][C:9]1[S:13][C:12]([C:14]([NH:16][CH:17]2[CH2:21][CH2:20][NH:19][CH2:18]2)=[O:15])=[CH:11][C:10]=1[N+:22]([O-:24])=[O:23].[CH:26]1(OCCO[Si](C)(C)C)[CH2:28][CH2:27]1.C(O)(=O)C.[C-]#N.[BH4-].[Na+]>CO>[CH:26]1([N:19]2[CH2:20][CH2:21][CH:17]([NH:16][C:14]([C:12]3[S:13][C:9]([S:8][C:7]4[C:6]([Cl:25])=[CH:5][N:4]=[CH:3][C:2]=4[Cl:1])=[C:10]([N+:22]([O-:24])=[O:23])[CH:11]=3)=[O:15])[CH2:18]2)[CH2:28][CH2:27]1
KomponentenVersuchsvorschriftAufarbeitungQuellen und NachweiseNotizen zur Reaktion

Komponenten

6

Edukt 4

HCID 176Acetic AcidHCID 57138593HCID 57138593, VerbindungHCID 60207421HCID 60207421, VerbindungHCID 131723130HCID 131723130, Verbindung

Produkt 1

HCID 60207424HCID 60207424, VerbindungAusbeute 5,4 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 887
Methanol
Lösungsmittel

Versuchsvorschrift

To a solution of 5-((3,5-dichloropyridin-4-yl)thio)-4-nitro-N-(pyrrolidin-3-yl)thiophene-2-carboxamide (0.20 g, 0.48 mmol), (2-cyclopropoxyethoxy)trimethylsilane (498 mg, 2.86 mmol) and acetic acid (286 mg, 4.77 mmol) in methanol (10 mL) under nitrogen, was added sodium borohydride cyanide powder (150 mg, 2.38 mmol) by small portion. The resulting reaction mixture was heated under reflux for 4 hours. After this time, the reaction mixture was passed through a celite cartridge and the organic solution was concentrated. The resulting residue was dissolved in ethyl acetate and was washed with sodium bicarbonate solution and brine. The organic layer was separated, dried (Na2SO4) and concentrated. The crude was purified by reverse phase HPLC to afford the titled product as a solid (12.0 mg, 5% yield) 1H NMR (400 MHz, d6-DMSO) δ: 8.99 (2H, m), 8.87 (1H, d), 8.54 (1H, s), 4.23 (1H, m), 2.83 (2H, m), 2.07 (1H, m), 1.63 (2H, m), 1.23 (2H, m), 0.48 (2H, m), 0.38 (2H, m). MS m/z: 459.08, 461.07 [M+H]+.

Aufarbeitung

  1. customThe resulting reaction mixture
  2. temperaturewas heated
  3. temperatureunder reflux for 4 hours
  4. concentrationthe organic solution was concentrated
  5. dissolutionThe resulting residue was dissolved in ethyl acetate
  6. washwas washed with sodium bicarbonate solution and brine
  7. customThe organic layer was separated
  8. dry with materialdried (Na2SO4)
  9. concentrationconcentrated
  10. customThe crude was purified by reverse phase HPLC

Quellen und Nachweise

ORD-Eintrag
ord-5afb45c4794443e9b599a5f0b115207c
Quelldatensatz
uspto-grants-2014_03
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US08680139B2

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