2-Amino-5-ethyl-1,3,4-thiadiazole → (2S,4S)-1-[[N-[4-[N-(5-ethyl-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile

HRID 228034

반응식

HRID 228034 반응식
[C:1]([C:4]12[CH2:11][CH2:10][C:7]([NH:12][CH2:13][C:14]([N:16]3[CH2:20][C@@H:19]([F:21])[CH2:18][C@H:17]3[C:22]#[N:23])=[O:15])([CH2:8][CH2:9]1)[CH2:6][CH2:5]2)(O)=[O:2].[NH2:24][C:25]1[S:26][C:27]([CH2:30][CH3:31])=[N:28][N:29]=1>>[CH2:30]([C:27]1[S:26][C:25]([NH:24][C:1]([C:4]23[CH2:11][CH2:10][C:7]([NH:12][CH2:13][C:14]([N:16]4[CH2:20][C@@H:19]([F:21])[CH2:18][C@H:17]4[C:22]#[N:23])=[O:15])([CH2:6][CH2:5]2)[CH2:8][CH2:9]3)=[O:2])=[N:29][N:28]=1)[CH3:31]

참가 물질

3

반응물 2

HCID 264442-Amino-5-ethyl-1,3,4-thiadiazoleHCID 57634365(2S,4S)-1-[[N-(4-carboxybicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile

생성물 1

HCID 57756789(2S,4S)-1-[[N-[4-[N-(5-ethyl-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile수율 51.8%

실험 절차

In a similar manner to Example 87, (2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (50.0 mg) and 2-amino-5-ethyl-1,3,4-thiadiazole (43.9 mg) were used to obtain (2S,4S)-1-[[N-[4-[N-(5-ethyl-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (34.8 mg).

출처 및 근거

ORD 기록
ord-1d3da2e351764757bbe578b9f01abab5
출처 데이터셋
uspto-grants-2009_07
특허 번호
US07560569B2

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