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参考文献:3-芳基-4-羟基喹啉-2(1H)-作为nmda /甘氨酸部位拮抗剂的5-,6-,7-和8-氮杂类似物的合成和sar.
标题:3-芳基-4-羟基喹啉-2(1H)-作为nmda /甘氨酸部位拮抗剂的5-,6-,7-和8-氮杂类似物的合成和sar.
摘要:合成了3-芳基-4-羟基喹啉-2(1H)-One的一系列5-,6-,7-和8-氮杂类似物,并测定为nmda /甘氨酸受体拮抗剂.这些拮抗剂的体外效能是通过在大鼠大脑皮膜中置换甘氨酸位点放射性配体[[(3)h] 5,7-Dicholorokynurenic酸([(3)h] Dcka)确定的.还使用表达克隆的nmda受体(nr)1A / 2C亚基的非洲爪蟾卵母细胞中的电生理测定法测试了所选化合物的功能拮抗作用.在研究的5,6,7,8氮杂-3-芳基-4-羟基喹啉2(1H)-中,5-氮杂7-氯-4-羟基-3-(3-苯氧基苯基))quinolin-2-(1H)-One(13I)是最有效的拮抗剂,在[(3)h] Dcka结合中的ic(50)值为110 Nm,在电生理学中的k(b)为11 Nm分析.
DOI:10.1016/s0968-0896(01)00115-8
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专利信息
专利号:US-3950160-A
优先权日:1972-09-27
标题:Inhibiting the growth of weeds with 2-substituted pyrdidopyimidines and salts thereof
发明人:ABU EL-HAJ MARWAN J; DOMINY BERYL WILLIAM
权利人:PFIZER
摘要:2-Substituted pyridopyrimidines and their alkali and alkylamine salts as herbicides, and processes for the synthesis of starting materials leading to the preparation thereof.
专利号:WO-2015036522-A1
优先权日:2013-09-13
标题:Process for the preparation and isolation of (s)-3-amino-n-cyclopropyl-2,2-dialkoxyhexanamide and (s)-tert-butyl(1-(cyclopropylamino)-2,2-dialkoxy-1-oxohexan-3-yl)carbamate and use thereof for the preparation of telaprevir
发明人:BARTH ROLAND; BENITO-GARAGORRI DAVID; WILHELM THORSTEN
权利人:SANDOZ AG
摘要:The present invention refers to processes for preparing (1 S ,3a R, 6aS)-2-[(2Sv)-2-[[(2S)-2- Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]- N -[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1 H -cyclopenta[c] pyrrol-1-carboxamid via novel cyclic anhydrides as intermediates. The cyclic anhydrides can easily be reacted with cyclopropylamine to provide the intermediates (S)-3-Amino- N -cyclopropyl-2,2-dialkoxyhexanamide and (S)-tert-Butyl (1-(cyclopropylamino)-2,2-dialkoxy-1-oxohexan-3-yl)carbamate. The present invention also refers to intermediates of the process for preparing telaprevir and processes for the synthesis of said intermediates.
专利号:US-3962264-A
优先权日:1972-09-27
标 题:Process for making 2-amino nicotinonitrile
发明人:ABU EL-HAJ MARWAN J; DOMINY BERYL WILLIAM
权利人:PFIZER
摘要:2-Substituted pyridopyrimidines and their alkali and alkylamine salts as herbicides, and processes for the synthesis of starting materials leading to the preparation thereof.
专利号:US-3917624-A
优先权日:1972-09-27
标题:Process for producing 2-amino-nicotinonitrile intermediates
发明人:ABU EL-HAJ MARWAN J; DOMINY BERYL WILLIAM
权利人:PFIZER
摘要:2-Substituted pyridopyrimidines and their alkali and alkylamine salts as herbicides, and processes for the synthesis of starting materials leading to the preparation thereof.
专利号:US-3862191-A
优先权日:1972-09-27
标 题 :Pyrido{8 2,3-d{9 pyrimidin-4(3H)-one
发明人:EL-HAJ MARWAN J ABU; DOMINY BERYL WILLIAM
权利人:PFIZER
摘要:2-Substituted pyridopyrimidines and their alkali and alkylamine salts as herbicides, and processes for the synthesis of starting materials leading to the preparation thereof.
专利号:CN-114805353-A
优先权日:2022-01-11
标题:Synthesis of azatryptanthrin derivative and application of azatryptanthrin derivative in prevention and treatment of plant pathogenic bacteria, fungi bactericide and anti-plant virus preparation