1-Acetylpiperazine → HCID 22053575, compound

HRID 1829667Notes

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

Participants

Reactant 2

HCID 837951-Acetylpiperazine

HCID 22053556HCID 22053556, compound

Product 1

HCID 22053575HCID 22053575, compoundYield 83%

Procedure

In a similar manner to Example 1, 6-[3,5-bis(trifluoromethyl)benzyl]-5,6,7,8,9,10-hexahydro-10-methyl-4-(2-methylphenyl)-2-(methylsulfonyl)-5-oxopyrimido[4,5-b][1,5]diazocine (Compound of Reference Example 21; 88.0 mg) was reacted with 1-acetylpiperazine (23.1 mg) to obtain 9-(4-acetylpiperazine-1-yl)-6-[3,5-bis(trifluoromethyl)benzyl]-5,6,7,8,9,10-hexahydro-10-methyl-4-(2-methylphenyl)-5-oxopyrimido[4,5-b][1,5]diazocine (78.6 mg, 83%).

Sources & evidence

ORD record: ord-dd371bddca9548aa840f21cd53eb1294
Source dataset: uspto-grants-2006_06
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US07064119B2

Reaction notes

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