苯磺酰氯 → tert-butyl N-[4-[[[(6S)-3-(benzenesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate

HRID 10967

反应方程式

HRID 10967 反应方程式
[C:1]([O:5][C:6](=[O:35])[NH:7][C:8](=[NH:34])[C:9]1[CH:14]=[CH:13][C:12]([CH2:15][NH:16][C:17]([C@H:19]2[N:23]3[C:24](=[O:33])[C:25]([NH:28][S:29]([CH3:32])(=[O:31])=[O:30])=[CH:26][N:27]=[C:22]3[CH2:21][CH2:20]2)=[O:18])=[CH:11][CH:10]=1)([CH3:4])([CH3:3])[CH3:2].C(OC(=O)NC([C:45]1[CH:50]=[CH:49]C(CNC([C@H]2N3C(=O)C(N)=CN=C3CC2)=O)=[CH:47][CH:46]=1)=N)(C)(C)C.C1(S(Cl)(=O)=O)C=CC=CC=1>>[C:1]([O:5][C:6](=[O:35])[NH:7][C:8](=[NH:34])[C:9]1[CH:14]=[CH:13][C:12]([CH2:15][NH:16][C:17]([C@H:19]2[N:23]3[C:24](=[O:33])[C:25]([NH:28][S:29]([C:32]4[CH:49]=[CH:50][CH:45]=[CH:46][CH:47]=4)(=[O:31])=[O:30])=[CH:26][N:27]=[C:22]3[CH2:21][CH2:20]2)=[O:18])=[CH:11][CH:10]=1)([CH3:4])([CH3:2])[CH3:3]

参与物

4

反应物 3

HCID 7369苯磺酰氯HCID 145857226tert-butyl N-[4-[[[(6S)-3-amino-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamateHCID 145857232tert-butyl N-[4-[[[(6S)-3-(methanesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate

产物 1

HCID 145857202tert-butyl N-[4-[[[(6S)-3-(benzenesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate收率 80.1%

实验过程

Following a procedure similar to that for the preparation of intermediate 16a, intermediate 1j (50 mg, 0.117 mmol) and benzene sulfonyl chloride (22.8 mg, 0.129 mmol) yielded 53.6 mg (80.1%) of intermediate 17a. MS (ESI) 567.0 (M+H+).

来源与证据

ORD记录
ord-d866ff3aac6341b991520d51ab1c5ea3
来源数据集
uspto-grants-2006_08
专利号
US07094783B2

关联笔记

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