Pyrazole → 2-Pyrazol-1-yl-quinazolin-8-ol

HRID 640791Notes

Reaction equation

HRID 640791 reaction equation
Cl[C:2]1[N:11]=[CH:10][C:9]2[C:4](=[C:5]([O:12]C)[CH:6]=[CH:7][CH:8]=2)[N:3]=1.[NH:14]1[CH:18]=[CH:17][CH:16]=[N:15]1.B(Br)(Br)Br>>[N:14]1([C:2]2[N:11]=[CH:10][C:9]3[C:4](=[C:5]([OH:12])[CH:6]=[CH:7][CH:8]=3)[N:3]=2)[CH:18]=[CH:17][CH:16]=[N:15]1

Participants

4

Reactant 3

HCID 1048PyrazoleHCID 25134Boron tribromideHCID 199886952-Chloro-8-methoxyquinazoline

Product 1

HCID 685622682-Pyrazol-1-yl-quinazolin-8-ol

Procedure

A mixture of the 2-chloride 113 (0.5 mmol) and pyrazole (2.5 mmol) was heated at 175° C. in a steel autoclave for 48 h. The crude product was then treated with BBr3 according to the procedure described in Example 6. Subsequent purification by column chromatography gave 2-pyrazol-1-yl-quinazolin-8-ol (A131).

Workup

  1. customSubsequent purification by column chromatography

Sources & evidence

ORD record
ord-79edada64f544434924c09e095eecdcc
Source dataset
uspto-grants-2010_04
Patent number
US07692011B2

Reaction notes

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