Thiomorpholine 1,1-dioxide → HCID 67157859, compound
Reaction equation
C(O[C:4]([C:6]1[N:7]=[N:8][C:9]([O:12][CH2:13][C:14]2[C:15]([C:20]3[CH:25]=[CH:24][C:23]([F:26])=[CH:22][CH:21]=3)=[N:16][O:17][C:18]=2[CH3:19])=[CH:10][CH:11]=1)=[O:5])C.[NH:27]1[CH2:32][CH2:31][S:30](=[O:34])(=[O:33])[CH2:29][CH2:28]1>>[O:33]=[S:30]1(=[O:34])[CH2:31][CH2:32][N:27]([C:4]([C:6]2[N:7]=[N:8][C:9]([O:12][CH2:13][C:14]3[C:15]([C:20]4[CH:21]=[CH:22][C:23]([F:26])=[CH:24][CH:25]=4)=[N:16][O:17][C:18]=3[CH3:19])=[CH:10][CH:11]=2)=[O:5])[CH2:28][CH2:29]1Participants
3
Procedure
As described for example 59, 6-[3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-pyridazine-3-carboxylic acid ethyl ester (143 mg, 0.4 mmol) was converted, using thiomorpholine-S,S-dioxide instead of aminomethylcyclopropane, to the title compound (131 mg, 73%) which was obtained as an off white solid. MS: m/e=447.1 [M+H]+.
Sources & evidence
- ORD record
- ord-cd9833b082bd4d0b93f061f2a7803038
- Source dataset
- uspto-grants-2011_05
- Patent number
- US07943619B2
Reaction notes
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