Triethylamine → 2-amino-6-fluoro-N-(5-fluoro-4-(4-((tetrahydro-2H-pyran-4-yl)sulfonyl)piperazin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

HRID 524931ノート

反応式

HRID 524931 の反応式
[O:1]1[CH2:6][CH2:5][CH:4]([S:7](Cl)(=[O:9])=[O:8])[CH2:3][CH2:2]1.[NH2:11][C:12]1[C:21]([C:22]([NH:24][C:25]2[CH:26]=[N:27][CH:28]=[C:29]([F:37])[C:30]=2[N:31]2[CH2:36][CH2:35][NH:34][CH2:33][CH2:32]2)=[O:23])=[C:15]2[N:16]=[CH:17][C:18]([F:20])=[CH:19][N:14]2[N:13]=1.CCN(CC)CC>CN(C=O)C>[NH2:11][C:12]1[C:21]([C:22]([NH:24][C:25]2[CH:26]=[N:27][CH:28]=[C:29]([F:37])[C:30]=2[N:31]2[CH2:36][CH2:35][N:34]([S:7]([CH:4]3[CH2:5][CH2:6][O:1][CH2:2][CH2:3]3)(=[O:9])=[O:8])[CH2:33][CH2:32]2)=[O:23])=[C:15]2[N:16]=[CH:17][C:18]([F:20])=[CH:19][N:14]2[N:13]=1

参加物

5

反応物 3

HCID 8471TriethylamineHCID 22637030Oxane-4-sulfonyl chlorideHCID 867209892-amino-6-fluoro-N-(5-fluoro-4-piperazin-1-yl-3-pyridyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

生成物 1

HCID 867209882-amino-6-fluoro-N-(5-fluoro-4-(4-((tetrahydro-2H-pyran-4-yl)sulfonyl)piperazin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

Tetrahydropyran-4-sulfonyl chloride (16.28 mg, 0.08815 mmol) was added to a suspension of 2-amino-6-fluoro-N-(5-fluoro-4-piperazin-1-yl-3-pyridyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide (30 mg, 0.08014 mmol) (synthesized according to the procedure similar to Example 2) and Et3N (12.16 mg, 16.75 μL, 0.1202 mmol) in DMF (0.2 mL). The crude mixture was purified by Fractionlynx HPLC. The clean aqueous fractions were combined and lyophilised, yielding 2-amino-6-fluoro-N-(5-fluoro-4-(4-((tetrahydro-2H-pyran-4-yl)sulfonyl)piperazin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide. MS (ES+) 523.1.

後処理

  1. customsynthesized
  2. customThe crude mixture was purified by Fractionlynx HPLC

出典と根拠

ORDレコード
ord-d8aeed86df614bb0861c85afc113320d
出典データセット
uspto-grants-2016_05
特許番号
US09340546B2

反応ノート

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