4-Fluorobenzenesulfonyl chloride → tert-butyl N-[4-[[[(6S)-3-[(4-fluorophenyl)sulfonylamino]-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate

HRID 10996

反応式

HRID 10996 の反応式
[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(C1C=CC(CNC([C@H]2N3C(=O)C(N(CC)CC)=CN=C3CC2)=O)=CC=1)=N)(C)(C)C.[F:71][C:72]1[CH:77]=[CH:76]C(S(Cl)(=O)=O)=[CH:74][CH:73]=1>>[C:1]([O:5][C:6](=[O:35])[NH:7][C:8]([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:76]=[CH:77][C:72]([F:71])=[CH:73][CH:74]=4)(=[O:31])=[O:30])=[CH:26][N:27]=[C:22]3[CH2:21][CH2:20]2)=[O:18])=[CH:11][CH:10]=1)=[NH:34])([CH3:4])([CH3:2])[CH3:3]

参加物

4

反応物 3

HCID 95884-Fluorobenzenesulfonyl chlorideHCID 145857232tert-butyl N-[4-[[[(6S)-3-(methanesulfonamido)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamateHCID 145857233tert-butyl N-[4-[[[(6S)-3-(diethylamino)-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate

生成物 1

HCID 145857220tert-butyl N-[4-[[[(6S)-3-[(4-fluorophenyl)sulfonylamino]-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carbonyl]amino]methyl]benzenecarboximidoyl]carbamate収率 41%

実験手順

Following a procedure similar to that for the preparation of 16a, intermediate 3a (50 mg, 0.117 mmol) and 4-fluorobenzene sulfonyl chloride (29.6 mg, 0.158 mmol) yielded 28.2 mg (41.0%) of 32a. MS (ESI) 585.0 (M+H+).

出典と根拠

ORDレコード
ord-de70dcd92b8a454b981be1181eb29201
出典データセット
uspto-grants-2006_08
特許番号
US07094783B2

関連ノート

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