10-methoxymethyl-8-chloromethyl-10H-pyrazino[2,3-b][1,4]benzothiazine → HCID 18670305, compound
Reaction equation
[CH3:1][O:2][CH2:3][N:4]1[C:9]2[CH:10]=[C:11](CCl)[CH:12]=[CH:13][C:8]=2[S:7][C:6]2[N:16]=[CH:17][CH:18]=[N:19][C:5]1=2.Cl.Cl.[NH2:22][CH2:23][CH2:24][C:25]1[N:26]=[CH:27][NH:28][CH:29]=1>>[NH2:22][CH2:23][CH2:24][C:25]1[N:26]=[CH:27][N:28]([C:11]2[CH:12]=[CH:13][C:8]3[S:7][C:6]4[N:16]=[CH:17][CH:18]=[N:19][C:5]=4[N:4]([CH2:3][O:2][CH3:1])[C:9]=3[CH:10]=2)[CH:29]=1Participants
3
Procedure
0.5 g of 10-methoxymethyl-8-chloromethyl-10H-pyrazino-[2,3-b][1,4]benzothiazine and 1.0 g of 4-(2-aminoethyl)imidazole dihydorchloride were treated by the same method as the one of Example 1094 to thereby give 0.7 g of crude 8-[4-(2-aminoethyl)imidazol-1-yl]-10-methoxymethyl-10H-pyrazino[2,3-b][1,4]benzothiazine as a brown solid. This crude product was then treated by the same method as the one of Example 316 to thereby give 0.1 g of N-[2-[1-(10-methoxymethyl-10H-pyrazino[2,3-b][1,4benzothiazin-8-ylmethyl)imidazol-4-yl]ethyl]methanesulfonamide. Further, it was treated by the same method as the one of Example 8 to thereby give 50 mg of the title compound as yellow crystals.
Sources & evidence
- ORD record
- ord-e9d0b59e605a435bb7a85e406ac015c8
- Source dataset
- uspto-grants-2003_02
- Patent number
- US06518423B1
Reaction notes
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