Hydrochloric Acid → Tetrahydro-pyran-4-carboxylic acid [7-aminomethyl-6-(2,4-dichloro-phenyl)-imidazo[1,2-a]pyridin-3-yl]-amide

HRID 420535ノート

反応式

HRID 420535 の反応式
C(OC(=O)[NH:7][CH2:8][C:9]1[C:14]([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][C:16]=2[Cl:22])=[CH:13][N:12]2[C:23]([NH:26][C:27]([CH:29]3[CH2:34][CH2:33][O:32][CH2:31][CH2:30]3)=[O:28])=[CH:24][N:25]=[C:11]2[CH:10]=1)(C)(C)C.Cl>O1CCOCC1>[NH2:7][CH2:8][C:9]1[C:14]([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][C:16]=2[Cl:22])=[CH:13][N:12]2[C:23]([NH:26][C:27]([CH:29]3[CH2:30][CH2:31][O:32][CH2:33][CH2:34]3)=[O:28])=[CH:24][N:25]=[C:11]2[CH:10]=1

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 57906481{6-(2,4-Dichloro-phenyl)-3-[(tetrahydro-pyran-4-carbonyl)-amino]-imidazo[1,2-a]pyridin-7-ylmethyl}-carbamic acid tert-butyl ester

生成物 1

HCID 57906482Tetrahydro-pyran-4-carboxylic acid [7-aminomethyl-6-(2,4-dichloro-phenyl)-imidazo[1,2-a]pyridin-3-yl]-amide収率 77.1%

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒2 回

実験手順

To a solution of {6-(2,4-dichloro-phenyl)-3-[(tetrahydro-pyran-4-carbonyl)-amino]-imidazo[1,2-a]pyridin-7-ylmethyl}-carbamic acid tert-butyl ester (79.5 mg, 0.153 mmol) in dioxane (3 mL) was added a 4M HCl solution in dioxane (2 mL) and the mixture was stirred at RT for 15 min. The formed precipitate was filtered and dried under vacuum to yield the title compound (2HCl salt, 58 mg, 0.118 mmol, 48%) as a brownish solid. MS: 419 [M+1]+; HPLC: AtRet=0.83.

後処理

  1. filtrationThe formed precipitate was filtered
  2. customdried under vacuum

出典と根拠

ORDレコード
ord-24070c377f5b4c25bbe34459ed13d069
出典データセット
uspto-grants-2012_01
特許番号
US08097617B2

反応ノート

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