Hydrochloric Acid → (3R)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 3-amino-4-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)butanoate

HRID 1752941ノート

反応式

HRID 1752941 の反応式
C(OC([NH:8][C@H:9]([CH2:26][C:27]1[CH:32]=[CH:31][C:30]([C:33]2[CH:38]=[C:37]([Cl:39])[CH:36]=[CH:35][C:34]=2[F:40])=[CH:29][CH:28]=1)[CH2:10][C:11]([O:13][CH:14]([O:16][C:17]([O:19][CH:20]1[CH2:25][CH2:24][CH2:23][CH2:22][CH2:21]1)=[O:18])[CH3:15])=[O:12])=O)(C)(C)C.Cl>O1CCOCC1>[NH2:8][C@H:9]([CH2:26][C:27]1[CH:28]=[CH:29][C:30]([C:33]2[CH:38]=[C:37]([Cl:39])[CH:36]=[CH:35][C:34]=2[F:40])=[CH:31][CH:32]=1)[CH2:10][C:11]([O:13][CH:14]([O:16][C:17]([O:19][CH:20]1[CH2:25][CH2:24][CH2:23][CH2:22][CH2:21]1)=[O:18])[CH3:15])=[O:12]

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 86729185(3R)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 3-((tert-butoxycarbonyl)amino)-4-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)butanoate

生成物 1

HCID 86729186(3R)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 3-amino-4-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)butanoate収率 104%

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒

反応条件

温度
23 °C

実験手順

To (3R)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 3-((tert-butoxycarbonyl)amino)-4-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)butanoate (2.02 g, 3.49 mmol) was added 9 mL of 4M HCl in 1,4-dioxane. The reaction mixture was stirred at 23° C. for approximately 1 hour. The reaction mixture was evaporated approximately to dryness to afford (3R)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 3-amino-4-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)butanoate (approximately 1.73 g, 104%) and taken directly to the next step. LCMS (ES+) C25H29ClFNO5: Calc.: 477.2; Found: 478.2[M+H]+.

後処理

  1. customThe reaction mixture was evaporated approximately to dryness

出典と根拠

ORDレコード
ord-bd8d39f79a344c59ba21a6e3ef51d668
出典データセット
uspto-grants-2015_10
特許番号
US09163040B2

反応ノート

読み込み中…