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Diisopropylethylamine → N-(2'-Oxo-1',2',5,7-tetrahydrospiro[cyclopenta[c]pyridine-6,3'-pyrrolo[2,3-b]pyridin]-3-yl)-2-[2-oxo-1'-(2,2,2-trifluoroethyl)spiro[indole-3,4'-piperidin]-1(2H)-yl]acetamide

HRID 1921224
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Reaktionsgleichung

Reaktionsgleichung von HRID 1921224
[O:1]=[C:2]1[C:10]2([CH2:15][CH2:14][N:13]([CH2:16][C:17]([F:20])([F:19])[F:18])[CH2:12][CH2:11]2)[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[N:3]1[CH2:21][C:22]([OH:24])=O.[NH2:25][C:26]1[N:31]=[CH:30][C:29]2[CH2:32][C:33]3([CH2:43][C:28]=2[CH:27]=1)[C:41]1[C:36](=[N:37][CH:38]=[CH:39][CH:40]=1)[NH:35][C:34]3=[O:42].C1CN(C(Cl)=[N+]2CCCC2)CC1.F[P-](F)(F)(F)(F)F.C(N(CC)C(C)C)(C)C>C1COCC1>[O:42]=[C:34]1[NH:35][C:36]2=[N:37][CH:38]=[CH:39][CH:40]=[C:41]2[C:33]21[CH2:32][C:29]1[CH:30]=[N:31][C:26]([NH:25][C:22](=[O:24])[CH2:21][N:3]3[C:4]4[C:9](=[CH:8][CH:7]=[CH:6][CH:5]=4)[C:10]4([CH2:15][CH2:14][N:13]([CH2:16][C:17]([F:18])([F:19])[F:20])[CH2:12][CH2:11]4)[C:2]3=[O:1])=[CH:27][C:28]=1[CH2:43]2
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Komponenten

6

Edukt 4

HCID 81531DiisopropylethylamineHCID 27366521-(Chloro-1-pyrrolidinylmethylene)pyrrolidinium HexafluorophosphateHCID 184493632-Oxo-1'-(2,2,2-trifluoroethyl)-spiro[indoline-3,4'-piperidine]-1-acetic acid2×HCID 57974077(+/-)-3-amino-5,7-dihydrospiro[cyclopenta[c]pyridine-6,3'-pyrrolo[2,3-b]pyridin]-2'(1'H)-one2×

Produkt 1

HCID 59279590
N-(2'-Oxo-1',2',5,7-tetrahydrospiro[cyclopenta[c]pyridine-6,3'-pyrrolo[2,3-b]pyridin]-3-yl)-2-[2-oxo-1'-(2,2,2-trifluoroethyl)spiro[indole-3,4'-piperidin]-1(2H)-yl]acetamide

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028TetrahydrofuranLösungsmittel

Versuchsvorschrift

A mixture of 2-oxo-1′-(2,2,2-trifluoroethyl)-spiro[indoline-3,4′-piperidine]-1-acetic acid (79 mg, 0.23 mmol, described in Intermediate 11), (±)-3-amino-5,7-dihydrospiro[cyclopenta[c]pyridine-6,3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one (71 mg, 0.28 mmol, described in Intermediate 3), N,N,N′,N′-bis(tetramethylene)chloroformamidinium hexafluorophosphate (153 mg, 0.46 mmol), and N,N-diisopropylethylamine (0.20 mL, 1.15 mmol) in THF (2 mL) is stirred at ambient temperature for 18 h. The reaction mixture is purified directly by HPLC using a reversed phase C18 column and eluting with a gradient of H2O:CH3CN:CF3CO2H—90:10:0.1 to 5:95:0.1. The pure, product-containing fractions are combined and made basic with saturated aqueous NaHCO3. The resulting mixture is extracted with EtOAc (3×20 mL), and the combined organic extracts are washed with brine, dried over Na2SO4, filtered, and concentrated in vacuo to provide the title compound.

Aufarbeitung

  1. customThe reaction mixture is purified directly by HPLC
  2. washeluting with a gradient of H2O
  3. additionThe pure, product-containing fractions
  4. extractionThe resulting mixture is extracted with EtOAc (3×20 mL)
  5. washthe combined organic extracts are washed with brine
  6. dry with materialdried over Na2SO4
  7. filtrationfiltered
  8. concentrationconcentrated in vacuo

Quellen und Nachweise

ORD-Eintrag
ord-9c49f4a579614886b5a06af357437340
Quelldatensatz
uspto-grants-2012_05
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US08173655B2

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