2-[6-(1H-indazol-6-ylcarbamoyl)-1H-benzimidazol-2-ylamino]-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester → 2-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-2-ylamino)-3H-benzimidazole-5-carboxylic acid (1H-indazol-6-yl)-amide

HRID 1163382ノート

反応式

HRID 1163382 の反応式
C(OC([N:8]1[CH2:13][CH2:12][C:11]2[N:14]=[C:15]([NH:17][C:18]3[NH:22][C:21]4[CH:23]=[C:24]([C:27](=[O:38])[NH:28][C:29]5[CH:37]=[C:36]6[C:32]([CH:33]=[N:34][NH:35]6)=[CH:31][CH:30]=5)[CH:25]=[CH:26][C:20]=4[N:19]=3)[S:16][C:10]=2[CH2:9]1)=O)(C)(C)C>CO.Cl.O1CCOCC1.CCOCC>[NH:35]1[C:36]2[C:32](=[CH:31][CH:30]=[C:29]([NH:28][C:27]([C:24]3[CH:25]=[CH:26][C:20]4[N:19]=[C:18]([NH:17][C:15]5[S:16][C:10]6[CH2:9][NH:8][CH2:13][CH2:12][C:11]=6[N:14]=5)[NH:22][C:21]=4[CH:23]=3)=[O:38])[CH:37]=2)[CH:33]=[N:34]1

参加物

6

反応物 1

HCID 595225562-[6-(1H-indazol-6-ylcarbamoyl)-1H-benzimidazol-2-ylamino]-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester

生成物 1

HCID 595225712-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-2-ylamino)-3H-benzimidazole-5-carboxylic acid (1H-indazol-6-yl)-amide

試薬・触媒・溶媒 4

HCID 313Hydrochloric Acid溶媒HCID 887Methanol溶媒HCID 3283Diethyl Ether溶媒HCID 312751,4-Dioxane溶媒

実験手順

To a solution of 2-[6-(1H-indazol-6-ylcarbamoyl)-1H-benzimidazol-2-ylamino]-6,7-dihydro-4H-thiazolo[5,4-c]pyridine-5-carboxylic acid tert-butyl ester (0.25 mmol; see Example 79) in methanol (1 mL), 4M HCl in dioxane (0.5 mL) was added. The resulting mixture was stirred at room temperature for 5-6 h. The volatiles were removed in vacuo, the residue obtained was suspended in ether. The solid obtained was collected by filtration, washed with ether and dried in vacuo to afford 2-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-2-ylamino)-3H-benzimidazole-5-carboxylic acid (1H-indazol-6-yl)-amide as a hydrochloride salt. MS: m/z 431 (M+H)+.

後処理

  1. customThe volatiles were removed in vacuo
  2. customthe residue obtained
  3. customThe solid obtained
  4. filtrationwas collected by filtration
  5. washwashed with ether
  6. customdried in vacuo

出典と根拠

ORDレコード
ord-85073f3181354267b8506e8783d7d0bb
出典データセット
uspto-grants-2010_10
特許番号
US07820821B2

反応ノート

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