Trifluoroacetic acid → 2-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(propyl-amino)pyridin-4-yl)phenoxy}ethyl L-alaninate trifluoroacetate

HRID 1621338ノート

反応式

HRID 1621338 の反応式
C(OC([NH:8][C@H:9]([C:11]([O:13][CH2:14][CH2:15][O:16][C:17]1[CH:22]=[CH:21][C:20]([C:23]2[C:28]([C:29]#[N:30])=[C:27]([NH:31][CH2:32][CH2:33][CH3:34])[N:26]=[C:25]([S:35][CH2:36][C:37]3[N:38]=[C:39]([C:42]4[CH:47]=[CH:46][C:45]([Cl:48])=[CH:44][CH:43]=4)[S:40][CH:41]=3)[C:24]=2[C:49]#[N:50])=[CH:19][CH:18]=1)=[O:12])[CH3:10])=O)(C)(C)C.[F:51][C:52]([F:57])([F:56])[C:53]([OH:55])=[O:54]>ClCCl>[F:51][C:52]([F:57])([F:56])[C:53]([OH:55])=[O:54].[NH2:8][C@H:9]([C:11]([O:13][CH2:14][CH2:15][O:16][C:17]1[CH:22]=[CH:21][C:20]([C:23]2[C:28]([C:29]#[N:30])=[C:27]([NH:31][CH2:32][CH2:33][CH3:34])[N:26]=[C:25]([S:35][CH2:36][C:37]3[N:38]=[C:39]([C:42]4[CH:47]=[CH:46][C:45]([Cl:48])=[CH:44][CH:43]=4)[S:40][CH:41]=3)[C:24]=2[C:49]#[N:50])=[CH:19][CH:18]=1)=[O:12])[CH3:10]

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 687654192-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(propylamino)pyridin-4-yl)phenoxy}ethyl N-(tert-butoxycarbonyl)-L-alaninate

生成物 1

HCID 468509402-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(propyl-amino)pyridin-4-yl)phenoxy}ethyl L-alaninate trifluoroacetate

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

873 mg (1.191 mmol) of 2-{4-(2-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(propylamino)pyridin-4-yl)phenoxy}ethyl N-(tert-butoxycarbonyl)-L-alaninate (Example 14A) were initially charged in 29 ml of dichloromethane. 1.84 ml (23.817 mmol) of trifluoroacetic acid were added, and the reaction solution was then stirred at RT overnight. The reaction solution was concentrated by evaporation and the residue was triturated with diethyl ether. The solid formed was filtered off and dried. This gave 914 mg (89% of theory) of the target compound.

後処理

  1. concentrationThe reaction solution was concentrated by evaporation
  2. customthe residue was triturated with diethyl ether
  3. customThe solid formed
  4. filtrationwas filtered off
  5. customdried

出典と根拠

ORDレコード
ord-b2b711c235554e2ca26ce6527e03ea4f
出典データセット
uspto-grants-2014_07
特許番号
US08772498B2

反応ノート

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