N'-Hydroxy-4-methylbenzenecarboximidamide → 4-({3-[3-(4-Methylphenyl)-1,2,4-oxadiazol-5-yl]-5-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-carbonyl)morpholine

HRID 1642914노트

반응식

HRID 1642914 반응식
[N:1]1([C:7]([N:9]2[CH2:14][CH:13]([C:15]3[CH:20]=[CH:19][C:18]([O:21][C:22]([F:25])([F:24])[F:23])=[CH:17][CH:16]=3)[CH2:12][CH:11]([C:26]([OH:28])=O)[CH2:10]2)=[O:8])[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.O[N:30]=[C:31]([C:33]1[CH:38]=[CH:37][C:36]([CH3:39])=[CH:35][CH:34]=1)[NH2:32]>>[CH3:39][C:36]1[CH:37]=[CH:38][C:33]([C:31]2[N:32]=[C:26]([CH:11]3[CH2:12][CH:13]([C:15]4[CH:20]=[CH:19][C:18]([O:21][C:22]([F:23])([F:25])[F:24])=[CH:17][CH:16]=4)[CH2:14][N:9]([C:7]([N:1]4[CH2:6][CH2:5][O:4][CH2:3][CH2:2]4)=[O:8])[CH2:10]3)[O:28][N:30]=2)=[CH:34][CH:35]=1

참가 물질

3

반응물 2

HCID 209113N'-Hydroxy-4-methylbenzenecarboximidamideHCID 580025001-(Morpholin-4-ylcarbonyl)-5-[4-(trifluoromethoxy)phenyl]piperidine-3-carboxylic acid

생성물 1

HCID 580027354-({3-[3-(4-Methylphenyl)-1,2,4-oxadiazol-5-yl]-5-[4-(trifluoromethoxy)phenyl]piperidin-1-yl}-carbonyl)morpholine

실험 절차

80 mg (0.20 mmol) of 1-(morpholin-4-ylcarbonyl)-5-[4-(trifluoromethoxy)phenyl]piperidine-3-carboxylic acid (Example 44A) and 33 mg (0.22 mmol, 1.1 eq.) of N′-hydroxy-4-methylbenzenecarboximidamide were reacted according to the General Method 1. Yield: 68 mg (66% of theory)

출처 및 근거

ORD 기록
ord-fa7e6c3e660942b58df47f675298473e
출처 데이터셋
uspto-grants-2012_02
특허 번호
US08119663B2

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