Morpholine → HCID 86682444, compound

HRID 715871Notes

Reaction equation

HRID 715871 reaction equation
[NH:1]1[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.[C:7]([C:10]1[CH:11]=[N:12][C:13]([N:16]2[CH2:21][CH2:20][CH:19]([C:22]3[C:31]([CH:32]([F:43])[C:33]4[CH:38]=[CH:37][C:36]([C:39]([F:42])([F:41])[F:40])=[CH:35][CH:34]=4)=[C:30]([CH:44]4[CH2:49][CH2:48][C:47]([F:51])([F:50])[CH2:46][CH2:45]4)[C:29]4[CH:28]([O:52]CC5C=CC(OC)=CC=5)[CH2:27][C:26]([CH3:63])([CH3:62])[CH2:25][C:24]=4[N:23]=3)[CH2:18][CH2:17]2)=[N:14][CH:15]=1)(O)=[O:8]>>[F:51][C:47]1([F:50])[CH2:46][CH2:45][CH:44]([C:30]2[C:29]3[CH:28]([OH:52])[CH2:27][C:26]([CH3:62])([CH3:63])[CH2:25][C:24]=3[N:23]=[C:22]([CH:19]3[CH2:18][CH2:17][N:16]([C:13]4[N:14]=[CH:15][C:10]([C:7]([N:1]5[CH2:6][CH2:5][O:4][CH2:3][CH2:2]5)=[O:8])=[CH:11][N:12]=4)[CH2:21][CH2:20]3)[C:31]=2[CH:32]([F:43])[C:33]2[CH:34]=[CH:35][C:36]([C:39]([F:40])([F:42])[F:41])=[CH:37][CH:38]=2)[CH2:49][CH2:48]1

Participants

3

Reactant 2

HCID 8083MorpholineHCID 86682443HCID 86682443, compound

Product 1

HCID 86682444HCID 86682444, compound

Procedure

Reactions similar to those of the second step of Reference Example 25 and Example 38 were performed except for using morpholine instead of methylamine aqueous solution, and from 70 mg of the crude product of 2-[1-(5-Carboxypyrimidin-2-yl)piperidin-4-yl]-4-(4,4-difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-5-[(4-methoxybenzyl)oxy]-7,7-dimethyl-5,6,7,8-tetrahydroquinoline, which was prepared in the first step of Reference Example 25, 27 mg of the title compound was obtained as a white solid (yield: 49%).

Sources & evidence

ORD record
ord-286f1c579fbc4945b622c2a7ca84197b
Source dataset
uspto-grants-2015_11
Patent number
US09187450B2

Reaction notes

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