2-(4-Fluorophenyl)-3-(2-methylsulfanyl-pyrimidin-4-yl)-3-oxo-propionic acid methyl ester → 1,2,3,4-Tetrahydrophthalazine
Reaction equation
N1C=CC(C2[N:19]3[N:10]([CH2:11][C:12]4[C:17]([CH2:18]3)=[CH:16][CH:15]=[CH:14][CH:13]=4)C(=O)C=2)=NC=1.COC(=O)C(C1C=CC(F)=CC=1)C(C1C=CN=C(SC)N=1)=O>>[CH2:11]1[C:12]2[C:17](=[CH:16][CH:15]=[CH:14][CH:13]=2)[CH2:18][NH:19][NH:10]1Participants
3
Procedure
The following scheme illustrates the assembly of the 3-pyrimidin-4-yl-5,10-dihydro-pyrazolo[1,2-b]phthalazine-1-one scaffold by the convergent step which condenses intermediates 3 and 5. The resulting intermediate is then transformed into the final compound having the selected R unit.
Sources & evidence
- ORD record
- ord-22e9abd4f1044d5e9f9d4171dfdb7c02
- Source dataset
- uspto-grants-2004_11
- Patent number
- US06821971B2
Reaction notes
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