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Diisopropylethylamine → N-[1-(2,6-Diethoxy-4'-fluoro-biphenyl-4-ylmethyl)-piperidin-4-yl]-3-hydroxy-5-methoxy-benzamide

HRID 502466
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HRID 502466 반응식
[CH2:1]([O:3][C:4]1[CH:5]=[C:6]([CH:26]=[C:27]([O:30][CH2:31][CH3:32])[C:28]=1F)[CH2:7][N:8]1[CH2:13][CH2:12][CH:11]([NH:14][C:15](=[O:25])[C:16]2[CH:21]=[C:20]([O:22][CH3:23])[CH:19]=[C:18]([OH:24])[CH:17]=2)[CH2:10][CH2:9]1)[CH3:2].C(OC1C=C(C=O)C=C(OCC)C=1[C:47]1[CH:52]=[CH:51][C:50]([F:53])=[CH:49][CH:48]=1)C.C([BH3-])#N.[Na+].C(N(C(C)C)C(C)C)C>C(O)C.C(O)(=O)C>[CH2:1]([O:3][C:4]1[CH:5]=[C:6]([CH2:7][N:8]2[CH2:9][CH2:10][CH:11]([NH:14][C:15](=[O:25])[C:16]3[CH:21]=[C:20]([O:22][CH3:23])[CH:19]=[C:18]([OH:24])[CH:17]=3)[CH2:12][CH2:13]2)[CH:26]=[C:27]([O:30][CH2:31][CH3:32])[C:28]=1[C:47]1[CH:52]=[CH:51][C:50]([F:53])=[CH:49][CH:48]=1)[CH3:2]
참가 물질실험 절차출처 및 근거반응 노트

참가 물질

7

반응물 4

HCID 81531DiisopropylethylamineHCID 5003444Sodium cyanoborohydrideHCID 593831002,6-Diethoxy-4'-fluoro-biphenyl-4-carbaldehydeHCID 68455428N-[1-(3,5-Diethoxy-4-fluoro-benzyl)-piperidin-4-yl]-3-hydroxy-5-methoxy-benzamide

생성물 1

HCID 68455814N-[1-(2,6-Diethoxy-4'-fluoro-biphenyl-4-ylmethyl)-piperidin-4-yl]-3-hydroxy-5-methoxy-benzamide

시약·촉매·용매

2
HCID 176Acetic Acid용매HCID 702Ethanol용매

실험 절차

In analogy to the procedure described in example 50k), 3-hydroxy-5-methoxy-N-piperidin-4-yl-benzamide hydrochloride (example 257) was reacted with 2,6-diethoxy-4′-fluoro-biphenyl-4-carbaldehyde (example 102), sodium cyanoborohydride, N-ethyl-diisopropylamine and acetic acid in ethanol at 50° C. to yield the title compound as colorless amorphous solid. MS: 523.3 (MH+).

출처 및 근거

ORD 기록
ord-a42fb093eb18487b9020f707d0f3f532
출처 데이터셋
uspto-grants-2010_08
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07772253B2

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