1-(Thien-2-ylcarbonyl)piperazine → 5-Oxo-7-[4-(thiophene-2-carbonyl)-piperazin-1-yl]-4,5-dihydro-2-thia-4-aza-indene-6-carbonitrile

HRID 902469노트

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HRID 902469 반응식
Cl[C:2]1[C:10]2[C:6](=[CH:7][S:8][CH:9]=2)[NH:5][C:4](=[O:11])[C:3]=1[C:12]#[N:13].[N:14]1([C:20]([C:22]2[S:23][CH:24]=[CH:25][CH:26]=2)=[O:21])[CH2:19][CH2:18][NH:17][CH2:16][CH2:15]1>>[O:11]=[C:4]1[C:3]([C:12]#[N:13])=[C:2]([N:17]2[CH2:18][CH2:19][N:14]([C:20]([C:22]3[S:23][CH:24]=[CH:25][CH:26]=3)=[O:21])[CH2:15][CH2:16]2)[C:10]2[C:6](=[CH:7][S:8][CH:9]=2)[NH:5]1

참가 물질

3

실험 절차

To yield a compound of structure (II) with R2 as carbonitrile, R3 as thiophene, and R1 as defined above, the intermediate 7-chloro-5-oxo-4,5-dihydro-2-thia-4-aza-indene-6-carbonitrile, depicted by formula (33), was reacted with piperazin-1-yl-thiophene-2-yl-methanone to yield 5-oxo-7-[4-(thiophene-2-carbonyl)-piperazin-1-yl]-4,5-dihydro-2-thia-4-aza-indene-6-carbonitrile, depicted by formula (34), which was either reacted with an appropriate halide (R1—X) or boronic acid (R1—B(OH)2) to yield target compounds of structure (II) with R2 as carbonitrile, R3 as thiophene, and R1 as defined above, as shown in Scheme 16.

출처 및 근거

ORD 기록
ord-8d94f9b940354829b11093ed20061b75
출처 데이터셋
uspto-grants-2008_04
특허 번호
US07365200B2

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