Triphenylphosphine → HCID 22563860, compound
Reaction equation
[CH:1]1(O)[CH2:5][CH2:4][CH:3]=[CH:2]1.[Cl:7][C:8]1[N:16]=[C:15]2[C:11]([NH:12][CH:13]=[N:14]2)=[C:10]([Cl:17])[N:9]=1.C1(P(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1.N(C(OCC)=O)=NC(OCC)=O>C1COCC1>[Cl:7][C:8]1[N:16]=[C:15]2[C:11]([N:12]=[CH:13][N:14]2[CH:1]2[CH2:5][CH2:4][CH:3]=[CH:2]2)=[C:10]([Cl:17])[N:9]=1Participants
6
Procedure
Add to a stirred solution of 2-cyclopenten-1-ol (2c 2.60 g, 30.9 mmol), 2,6-dichloropurine (1, 7.00 g, 37.0 mmol) and triphenyl phosphine (9.70 g, 37.0 mmol) in dry THF (120 ml) at 0° C., diethyl azodicarboxylate (5.85 ml, 37.0 mmol) dropwise over a period of 15 min. under a nitrogen atmosphere. Stir the resulting solution for 60 hrs at room temperature. Concentrate the reaction mixture, charge the residue directly onto a silica gel column and elute with hexane:ethyl acetate (3:1) to give of 2,6-dichloro-9-cyclopent-2-enyl-9H-purine (3c) (3.20 g, 41%.)
Workup
- concentrationConcentrate the reaction mixture
- additioncharge the residue directly onto a silica gel column
- washelute with hexane:ethyl acetate (3:1)
Sources & evidence
- ORD record
- ord-0167ac65c2af4e35ace4fd5d5e64ec48
- Source dataset
- uspto-grants-2008_09
- Patent number
- US07429595B2
Reaction notes
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