Ethyl Acetate → N1-[(1S,2R)-3-amino-1-(3,5-difluorobenzyl)-2-hydroxypropyl]-5-methyl-N3,N3-dipropylisophthalamide Acetic Acid Salt

HRID 348807

반응식

HRID 348807 반응식
[N:1]([CH2:4][C@@H:5]([OH:35])[C@@H:6]([NH:16][C:17](=[O:34])[C:18]1[CH:32]=[C:31]([CH3:33])[CH:30]=[C:20]([C:21]([N:23]([CH2:27][CH2:28][CH3:29])[CH2:24][CH2:25][CH3:26])=[O:22])[CH:19]=1)[CH2:7][C:8]1[CH:13]=[C:12]([F:14])[CH:11]=[C:10]([F:15])[CH:9]=1)=[N+]=[N-].[C:36]([O:39]CC)(=[O:38])[CH3:37]>C(O)(=O)C.[Pd]>[C:36]([OH:39])(=[O:38])[CH3:37].[NH2:1][CH2:4][C@@H:5]([OH:35])[C@@H:6]([NH:16][C:17](=[O:34])[C:18]1[CH:32]=[C:31]([CH3:33])[CH:30]=[C:20]([C:21]([N:23]([CH2:24][CH2:25][CH3:26])[CH2:27][CH2:28][CH3:29])=[O:22])[CH:19]=1)[CH2:7][C:8]1[CH:13]=[C:12]([F:14])[CH:11]=[C:10]([F:15])[CH:9]=1

참가 물질

5

반응물 2

HCID 8857Ethyl AcetateHCID 86585849N1-[(1S,2R)-3-azido-1-(3,5-difluorobenzyl)-2-hydroxypropyl]5-methyl-N3,N3-dipropylisophthalamide

생성물 1

HCID 68609581N1-[(1S,2R)-3-amino-1-(3,5-difluorobenzyl)-2-hydroxypropyl]-5-methyl-N3,N3-dipropylisophthalamide Acetic Acid Salt

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 176Acetic Acid용매

실험 절차

N1-[(1S,2R)-3-azido-1-(3,5-difluorobenzyl)-2-hydroxypropyl]5-methyl-N3,N3-dipropylisophthalamide (XV, EXAMPLE 167, 0.3 g, 0.62 mmole) in ethyl acetate (20 ml) and acetic acid (5 ml) is placed in a Parr pressure bottle. Palladium on carbon (10%, 5 g) is added and the mixture shaken under hydrogen at 50 psi for 2 hours. The mixture is filtered through a diatomaceous earth and the filtrate is concentrated to give the title compound; MS (MH+)=462.

후처리

  1. filtrationThe mixture is filtered through a diatomaceous earth
  2. concentrationthe filtrate is concentrated

출처 및 근거

ORD 기록
ord-3685fd0776a049499f685b5d75d3d938
출처 데이터셋
uspto-grants-2007_02
특허 번호
US07176242B2

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