Ammonia → 1-[2-(2-Chloro-benzylamino)-pyrido[4,3-d]pyrimidin-5-yl]-piperidine-4-carboxylic acid ethyl ester

HRID 41483Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 41483
[Cl:1][C:2]1[CH:20]=[CH:19][CH:18]=[CH:17][C:3]=1[CH2:4][NH:5][C:6]1[N:7]=[CH:8][C:9]2[C:15](Cl)=[N:14][CH:13]=[CH:12][C:10]=2[N:11]=1.[CH2:21]([O:23][C:24]([CH:26]1[CH2:31][CH2:30][NH:29][CH2:28][CH2:27]1)=[O:25])[CH3:22].N.O>C1COCC1>[CH2:21]([O:23][C:24]([CH:26]1[CH2:31][CH2:30][N:29]([C:15]2[C:9]3[CH:8]=[N:7][C:6]([NH:5][CH2:4][C:3]4[CH:17]=[CH:18][CH:19]=[CH:20][C:2]=4[Cl:1])=[N:11][C:10]=3[CH:12]=[CH:13][N:14]=2)[CH2:28][CH2:27]1)=[O:25])[CH3:22]

Komponenten

6

Edukt 4

HCID 222AmmoniaHCID 962WaterHCID 70770Ethyl 4-piperidinecarboxylateHCID 58450134(2-Chloro-benzyl)-(5-chloro-pyrido[4,3-d]pyrimidin-2-yl)-amine

Produkt 1

HCID 584501201-[2-(2-Chloro-benzylamino)-pyrido[4,3-d]pyrimidin-5-yl]-piperidine-4-carboxylic acid ethyl ester

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028TetrahydrofuranLösungsmittel

Reaktionsbedingungen

Temperatur
100 °C

Versuchsvorschrift

(2-Chloro-benzyl)-(5-chloro-pyrido[4,3-d]pyrimidin-2-yl)-amine 9 (500 mg, 1.64 mmol), Piperidine-4-carboxylic acid ethyl ester 12 (0.51 mL, 3.28 mmol) and NH3 (25% solution in water, 0.22 mL, 3.28 mmol) were dissolved in THF (5 mL) and stirred at 100° C. in a high pressure flask for 15 hours. To the mixture water (5 mL) was added and the precipitate formed was filtered off and dried in vacuo. The obtained colorless solid (583 mg, 1.37 mmol, 84%) was used without further purification.

Aufarbeitung

  1. customthe precipitate formed
  2. filtrationwas filtered off
  3. customdried in vacuo

Quellen und Nachweise

ORD-Eintrag
ord-1172c2765278437091facd59836387e8
Quelldatensatz
uspto-grants-2013_09
Patentnummer
US08530650B2

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