Formic Acid → N-[[5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5,8-diazaspiro[2.5]octan-8-yl]sulfonyl]formamide
Reaktionsgleichung
[CH:1]([OH:3])=O.N1(C(N2C=CN=C2)=O)C=CN=C1.C(OC([N:23]1[C:27]2[N:28]=[CH:29][N:30]=[C:31]([N:32]3[CH2:39][C:36]4([CH2:38][CH2:37]4)[N:35]([S:40](=[O:43])(=[O:42])[NH2:41])[CH2:34][CH2:33]3)[C:26]=2[CH:25]=[CH:24]1)=O)(C)(C)C.C1CCN2C(=NCCC2)CC1>C1COCC1>[N:28]1[C:27]2[NH:23][CH:24]=[CH:25][C:26]=2[C:31]([N:32]2[CH2:33][CH2:34][N:35]([S:40]([NH:41][CH:1]=[O:3])(=[O:43])=[O:42])[C:36]3([CH2:38][CH2:37]3)[CH2:39]2)=[N:30][CH:29]=1Komponenten
6
Edukt 4
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Reaktionsbedingungen
- Temperatur
- 50 °C
Versuchsvorschrift
Formic acid (0.24 mmol) was dissolved in dry THF (0.5 mL), added di(imidazol-1-yl)methanone (0.29 mmol) and then stirred at 50° C. for 30 min. before being cooled to rt and added 4-(4-Sulfamoyl-4,7-diaza-spiro[2.5]oct-7-yl)-pyrrolo[2,3-d]pyrimidine-7-carboxylic acid tert-butyl ester (Intermediate 2) (0.24 mmol) and DBU (0.29 mmol). The reaction mixture was stirred at rt for 16 h. The pure compounds were obtained by standard preparative HPLC purification of the reaction mixture.
Aufarbeitung
- temperaturebefore being cooled to rt
- stirringThe reaction mixture was stirred at rt for 16 h
- customThe pure compounds were obtained by standard preparative HPLC purification of the reaction mixture
Quellen und Nachweise
- ORD-Eintrag
- ord-a9a176899a204ca3955e49f5b575f145
- Quelldatensatz
- uspto-grants-2016_01
- Patentnummer
- US09233964B2
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