p-Toluenesulfonic acid monohydrate → 4-Amino-3-{5-[1-(4-chloro-benzyl)-1h-[1,2,3]triazol-4-yl]-2-methyl-phenoxymethyl}-thieno[3,2-c]pyridine-7-carboxylic acid (2-hydroxy-ethyl)-amide toluene-4-sulfonic acid salt

HRID 2081096노트

반응식

HRID 2081096 반응식
[OH:1][CH2:2][CH2:3][NH:4][C:5]([C:7]1[C:8]2[S:16][CH:15]=[C:14]([CH2:17][O:18][C:19]3[CH:24]=[C:23]([C:25]4[N:26]=[N:27][N:28]([CH2:30][C:31]5[CH:36]=[CH:35][C:34]([Cl:37])=[CH:33][CH:32]=5)[CH:29]=4)[CH:22]=[CH:21][C:20]=3[CH3:38])[C:9]=2[C:10]([NH2:13])=[N:11][CH:12]=1)=[O:6].O.[C:40]1([CH3:50])[CH:45]=[CH:44][C:43]([S:46]([OH:49])(=[O:48])=[O:47])=[CH:42][CH:41]=1>CO>[C:40]1([CH3:50])[CH:41]=[CH:42][C:43]([S:46]([OH:49])(=[O:47])=[O:48])=[CH:44][CH:45]=1.[OH:1][CH2:2][CH2:3][NH:4][C:5]([C:7]1[C:8]2[S:16][CH:15]=[C:14]([CH2:17][O:18][C:19]3[CH:24]=[C:23]([C:25]4[N:26]=[N:27][N:28]([CH2:30][C:31]5[CH:32]=[CH:33][C:34]([Cl:37])=[CH:35][CH:36]=5)[CH:29]=4)[CH:22]=[CH:21][C:20]=3[CH3:38])[C:9]=2[C:10]([NH2:13])=[N:11][CH:12]=1)=[O:6]

참가 물질

4

반응물 2

HCID 521998p-Toluenesulfonic acid monohydrateHCID 24810239HCID 24810239, 화합물

생성물 1

HCID 248102404-Amino-3-{5-[1-(4-chloro-benzyl)-1h-[1,2,3]triazol-4-yl]-2-methyl-phenoxymethyl}-thieno[3,2-c]pyridine-7-carboxylic acid (2-hydroxy-ethyl)-amide toluene-4-sulfonic acid salt

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

To solution of 4-amino-3-{5-[1-(4-chloro-benzyl)-1H-[1,2,3]triazol-4-yl]-2-methyl-phenoxymethyl}-thieno[3,2-c]pyridine-7-carboxylic acid (2-hydroxy-ethyl)-amide (0.159 g, 0.29 mmol) (from Example 37 supra) in methanol (10 mL) was treated with toluene-4-sulfonic acid hydrate (61.0 mg, 0.319 mmol) and heated at room temperature for 40 minutes. The solution was concentrated. The residue washed with diethyl ether, dissolved in water and lyophilized to 4-amino-3-{5-[1-(4-chloro-benzyl)-1H-[1,2,3]triazol-4-yl]-2-methyl-phenoxymethyl}-thieno[3,2-c]pyridine-7-carboxylic acid (2-hydroxy-ethyl)-amide 1.5 toluene-4-sulfonic acid salt. (Yield 0.21 g, 100%).

후처리

  1. concentrationThe solution was concentrated
  2. washThe residue washed with diethyl ether
  3. dissolutiondissolved in water

출처 및 근거

ORD 기록
ord-bf7c645fb7fd4a84baa4983e314a66c4
출처 데이터셋
uspto-grants-2011_04
특허 번호
US07932390B2

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