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Triethylamine → 2-Amino-N-(4-(4-fluoro-benzyloxy)-benzyl)-6-methoxymethyl-nicotinamide

HRID 2080181
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HRID 2080181 반응식
[NH2:1][C:2]1[N:10]=[C:9]([CH2:11][O:12][CH3:13])[CH:8]=[CH:7][C:3]=1[C:4]([OH:6])=O.[F:14][C:15]1[CH:30]=[CH:29][C:18]([CH2:19][O:20][C:21]2[CH:28]=[CH:27][C:24]([CH2:25][NH2:26])=[CH:23][CH:22]=2)=[CH:17][CH:16]=1.F[P-](F)(F)(F)(F)F.N1(O[P+](N(C)C)(N(C)C)N(C)C)C2C=CC=CC=2N=N1.C(N(CC)CC)C>CN(C)C=O.O>[NH2:1][C:2]1[N:10]=[C:9]([CH2:11][O:12][CH3:13])[CH:8]=[CH:7][C:3]=1[C:4]([NH:26][CH2:25][C:24]1[CH:27]=[CH:28][C:21]([O:20][CH2:19][C:18]2[CH:29]=[CH:30][C:15]([F:14])=[CH:16][CH:17]=2)=[CH:22][CH:23]=1)=[O:6]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

7

반응물 4

HCID 8471TriethylamineHCID 151348Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 64866744-(4-Fluoro-benzyloxy)-benzylamineHCID 231304372-Amino-6-methoxymethylnicotinic acid

생성물 1

HCID 231305542-Amino-N-(4-(4-fluoro-benzyloxy)-benzyl)-6-methoxymethyl-nicotinamide수율 60%

시약·촉매·용매 2

HCID 962Water용매HCID 6228Dimethylformamide용매

실험 절차

To a solution of 2-amino-6-methoxymethyl-nicotinic acid described in Preparation Example A-11 (10 mg, 0.055 mmol) and 4-(4-fluoro-benzyloxy)-benzylamine described in Preparation Example 155 (19 mg, 0.082 mmol) in N,N-dimethylformamide (1 mL) were added benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (29 mg, 0.066 mmol) and triethylamine (0.022 mL, 0.16 mmol), and the solution was stirred overnight at room temperature. Water was added to the reaction solution, the precipitated solid was filtered, and the title compound (13 mg, 0.033 mmol, 60%) was obtained as a colorless solid.

후처리

  1. filtrationthe precipitated solid was filtered

출처 및 근거

ORD 기록
ord-7054defe393149a792676bb55fd881e8
출처 데이터셋
uspto-grants-2011_04
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07932272B2

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