Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) → HCID 90295617、化合物

反応式

[O:1]=[C:2]1[N:6]2[C:7]3[CH:14]=[CH:13][C:12]([N:15]4[CH2:20][CH2:19][O:18][CH2:17][C:16]4=[O:21])=[CH:11][C:8]=3[O:9][CH2:10][C@H:5]2[C@H:4]([C:22]([OH:24])=O)[O:3]1.Cl.[Cl:26][C:27]1[S:31][C:30]([NH2:32])=[CH:29][CH:28]=1.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>>[Cl:26][C:27]1[S:31][C:30]([NH:32][C:22]([C@H:4]2[C@H:5]3[N:6]([C:7]4[CH:14]=[CH:13][C:12]([N:15]5[CH2:20][CH2:19][O:18][CH2:17][C:16]5=[O:21])=[CH:11][C:8]=4[O:9][CH2:10]3)[C:2](=[O:1])[O:3]2)=[O:24])=[CH:29][CH:28]=1

参加物

反応物 3

HCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)

HCID 665706625-Chlorothiophen-2-amine--hydrogen chloride (1/1)

HCID 90295836HCID 90295836、化合物

生成物 1

HCID 90295617HCID 90295617、化合物収率 60.34%

実験手順

Using compound (3R,3 aS)-1-oxo-7-(3-oxomorpholin-4-yl)-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-carboxylic acid (90 mg, 0.269 mmol), 5-chlorothiophene-2-amine hydrochloride (55 mg, 0.323 mmol), HATU (154 mg, 0.404 mmol), and TEA (95.3 mg, 0.943 mmol) as starting materials, preparation following the method as described in Example 11 (g) afforded white solid 73 mg, yield: 60.34%.