1-Acetylpiperazine → HCID 22053576, compound

HRID 1829651Notes

Reaction equation

[F:1][C:2]([F:40])([F:39])[C:3]1[CH:4]=[C:5]([CH:32]=[C:33]([C:35]([F:38])([F:37])[F:36])[CH:34]=1)[CH2:6][N:7]1[CH2:14][CH2:13][CH2:12][NH:11][C:10]2[N:15]=[C:16](S(C)(=O)=O)[N:17]=[C:18]([C:19]3[CH:24]=[CH:23][CH:22]=[CH:21][C:20]=3[O:25][CH3:26])[C:9]=2[C:8]1=[O:31].[C:41]([N:44]1[CH2:49][CH2:48][NH:47][CH2:46][CH2:45]1)(=[O:43])[CH3:42]>>[C:41]([N:44]1[CH2:49][CH2:48][N:47]([C:16]2[N:17]=[C:18]([C:19]3[CH:24]=[CH:23][CH:22]=[CH:21][C:20]=3[O:25][CH3:26])[C:9]3[C:8](=[O:31])[N:7]([CH2:6][C:5]4[CH:4]=[C:3]([C:2]([F:40])([F:1])[F:39])[CH:34]=[C:33]([C:35]([F:36])([F:38])[F:37])[CH:32]=4)[CH2:14][CH2:13][CH2:12][NH:11][C:10]=3[N:15]=2)[CH2:46][CH2:45]1)(=[O:43])[CH3:42]

Participants

Reactant 2

HCID 837951-Acetylpiperazine

HCID 22053555HCID 22053555, compound

Product 1

HCID 22053576HCID 22053576, compoundYield 81%

Procedure

In a similar manner to Example 1, 6-[3,5-bis(trifluoromethyl)benzyl]-5,6,7,8,9,10-hexahydro-4-(2-methoxyphenyl)-2-(methylsulfonyl)-5-oxopyrimido[4,5-b][1,5]diazocine (Compound of Reference Example 18; 88.3 mg) was reacted with 1-acetylpiperazine (23.1 mg) to obtain 2-(4-acetylpiperazine-1-yl)-6-[3,5-bis(trifluoromethyl)benzyl]-5,6,7,8,9,10-hexahydro-4-(2-methoxyphenyl)-5-oxopyrimido[4,5-b][1,5]diazocine (77.3 mg, 81%).

Sources & evidence

ORD record: ord-f362408ce6494a6b8106e4b1f011f429
Source dataset: uspto-grants-2006_06
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US07064119B2

Reaction notes

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