1-(2-Hydroxyethyl)piperazine → HCID 86750817, compound

HRID 1780225Notes

Reaction equation

HRID 1780225 reaction equation
[Cl:1]C[C@H:3]1[C:7]2=[C:8]3[C:12](=[C:13](O)[CH:14]=[C:6]2[N:5](C(C2NC4C(C=2)=CC(NC(C2OC5C(OC)=CC=CC=5C=2)=O)=CC=4)=O)[CH2:4]1)[NH:11][C:10]([C:16]([F:19])([F:18])[F:17])=[C:9]3[C:20]([O:22]C)=[O:21].OCCN1CCNCC1>>[ClH:1].[F:19][C:16]([F:17])([F:18])[C:10]1[NH:11][C:12]2[C:8]([C:9]=1[C:20]([OH:22])=[O:21])=[C:7]1[CH2:3][CH2:4][NH:5][C:6]1=[CH:14][CH:13]=2

Participants

3

Reactant 2

HCID 76771-(2-Hydroxyethyl)piperazineHCID 10842265HCID 10842265, compound

Product 1

HCID 86750817HCID 86750817, compound

Procedure

Methyl (1S)-1-chloromethyl-5-[4-(2-hydroxyethyl)piperazin-1-ylcarbonyl)oxy-3-[5-(7-methoxybenzofuran-2-ylcarbonyl)amino]-1H-indol-2-ylcarbonyl]-7-trifluoromethyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-8-carboxylate hydrochloride was prepared by using 25.6 mg (37 μmol) of methyl (1S)-1-chloromethyl-5-hydroxy-3-[5-(7-methoxybenzofuran-2-ylcarbonyl)amino-1H-indol-2-ylcarbonyl]-7-trifluoromethyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-8-carboxylate and 6.8 μl (56 μmol) of 1-(2-hydroxyethyl)piperazine in the same manner as in Example 46 in a yield of 22.2 mg (69%).

Sources & evidence

ORD record
ord-c31dfc3c01054a459ca696fed55b82d0
Source dataset
uspto-grants-1997_05
Patent number
US05629430

Reaction notes

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