Hydrochloric Acid → (S)-2-amino-3-hydroxy-N-{2-[4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)thiazol-2-yl]ethyl}propionamide

HRID 1401866ノート

反応式

HRID 1401866 の反応式
Cl.C(OC(=O)[NH:8][C@H:9]([C:12](=[O:35])[NH:13][CH2:14][CH2:15][C:16]1[S:17][CH:18]=[C:19]([C:21]2[CH:30]=[CH:29][C:28]3[C:27]([CH3:32])([CH3:31])[CH2:26][CH2:25][C:24]([CH3:34])([CH3:33])[C:23]=3[CH:22]=2)[N:20]=1)[CH2:10][OH:11])(C)(C)C>O1CCOCC1>[NH2:8][C@@H:9]([CH2:10][OH:11])[C:12]([NH:13][CH2:14][CH2:15][C:16]1[S:17][CH:18]=[C:19]([C:21]2[CH:30]=[CH:29][C:28]3[C:27]([CH3:32])([CH3:31])[CH2:26][CH2:25][C:24]([CH3:34])([CH3:33])[C:23]=3[CH:22]=2)[N:20]=1)=[O:35]

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 67324809((S)-2-hydroxy-1-{2-[4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)thiazol-2-yl]ethylcarbamoyl}ethyl)carbamic acid tert-butyl ester

生成物 1

HCID 67322250(S)-2-amino-3-hydroxy-N-{2-[4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)thiazol-2-yl]ethyl}propionamide

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒

実験手順

The protecting group is cleaved off as already described using HCl in dioxane starting from 82 mg (0.16 mmol) of ((S)-2-hydroxy-1-{2-[4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)thiazol-2-yl]ethylcarbamoyl}ethyl)carbamic acid tert-butyl ester from step c. The product is purified by means of preparative HPLC and is in the form of the formate.

後処理

  1. customThe product is purified by means of preparative HPLC

出典と根拠

ORDレコード
ord-b8317bcc5a754a2589d1ad8df4e5e953
出典データセット
uspto-grants-2014_12
特許番号
US08907098B2

反応ノート

読み込み中…