1,2-Benzenedicarbonitrile, 4-amino- → HCID 178462398, Verbindung

HRID 480961

Reaktionsgleichung

Reaktionsgleichung von HRID 480961
[NH2:1][C:2]1[CH:3]=[C:4]([C:10]#[N:11])[C:5](=[CH:8][CH:9]=1)[C:6]#[N:7].C[Al](C)C.[F:16][C:17]1[CH:22]=[C:21]([F:23])[CH:20]=[CH:19][C:18]=1[C@@:24]([OH:50])([CH2:44][N:45]1[CH:49]=[N:48][CH:47]=[N:46]1)[C@H:25]([S:27][C@@H:28]1[CH2:33][O:32][C@@H:31]([C:34]2[CH:43]=[CH:42][C:37]([C:38](OC)=[O:39])=[CH:36][CH:35]=2)[O:30][CH2:29]1)[CH3:26]>>[C:10]([C:4]1[CH:3]=[C:2]([CH:9]=[CH:8][C:5]=1[C:6]#[N:7])[NH:1][C:38](=[O:39])[C:37]1[CH:42]=[CH:43][C:34]([C@H:31]2[O:30][CH2:29][C@H:28]([S:27][C@H:25]([CH3:26])[C@:24]([C:18]3[CH:19]=[CH:20][C:21]([F:23])=[CH:22][C:17]=3[F:16])([OH:50])[CH2:44][N:45]3[CH:49]=[N:48][CH:47]=[N:46]3)[CH2:33][O:32]2)=[CH:35][CH:36]=1)#[N:11]

Komponenten

4

Edukt 3

HCID 925291,2-Benzenedicarbonitrile, 4-amino-HCID 16682925TrimethylaluminumHCID 178497884HCID 178497884, Verbindung

Produkt 1

HCID 178462398HCID 178462398, VerbindungAusbeute 71 %

Versuchsvorschrift

In the same manner as that described in Example 3(4), a reaction was carried out using commercially available 4-aminophthalonitrile (170 mg, 1.2 mmol), trimethylaluminium (1.1 ml, 1.07M n-hexane solution, 1.2 mmol) and methyl 4-[trans-5-[[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]thio]-1,3-dioxan-2-yl]benzoate (150 mg, 0.30 mmol), obtained in Example 12(1), and the reaction mixture was treated using a similar procedure to that described in Example 3(4) to afford the title compound (129 mg, yield 71%) as a yellow oil which was recrystallized from ethyl acetate-hexane to give pale yellow powdery crystals.

Aufarbeitung

  1. customobtained in Example 12(1)
  2. additionthe reaction mixture was treated

Quellen und Nachweise

ORD-Eintrag
ord-111708407deb490b9a820a19078cab2f
Quelldatensatz
uspto-grants-2003_11
Patentnummer
US06653330B2

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