Hydrochloric Acid → (R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-oxo-1,2-dihydropyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide

HRID 1426933ノート

反応式

HRID 1426933 の反応式
Cl.[Cl:2][CH2:3][CH2:4][CH2:5][N:6]([CH3:32])[C:7]([C:9]1[CH:10]=[N:11][N:12]2[CH:17]=[CH:16][C:15]([N:18]3[CH2:22][CH2:21][CH2:20][C@@H:19]3[C:23]3[C:24]([O:30]C)=[N:25][CH:26]=[C:27]([F:29])[CH:28]=3)=[N:14][C:13]=12)=[O:8]>C(#N)C>[Cl:2][CH2:3][CH2:4][CH2:5][N:6]([CH3:32])[C:7]([C:9]1[CH:10]=[N:11][N:12]2[CH:17]=[CH:16][C:15]([N:18]3[CH2:22][CH2:21][CH2:20][C@@H:19]3[C:23]3[C:24](=[O:30])[NH:25][CH:26]=[C:27]([F:29])[CH:28]=3)=[N:14][C:13]=12)=[O:8]

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 67470673(R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide

生成物 1

HCID 67470639(R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-oxo-1,2-dihydropyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide収率 150%

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

反応条件

温度
90 °C

実験手順

A mixture of HCl (4 N dioxane, 4 mL, 16.0 mmol) and (R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (100 mg, 0.224 mmol) was sealed in a pressure tube and heated at 90° C. for 90 minutes. The reaction mixture was then diluted with acetonitrile and concentrated to yield the crude product, which was carried to the next step without further purification (145 mg, 150% yield). MS (apci) m/z=433.0 (M+H).

後処理

  1. customwas sealed in a pressure tube
  2. concentrationconcentrated

出典と根拠

ORDレコード
ord-31017785c4ea47febdb8ff02f667690d
出典データセット
uspto-grants-2015_01
特許番号
US08933084B2

反応ノート

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