CAS: 78756-03-3; Ethyl 5,6-Dihydro-5-Methyl-6-Oxo-4H-Imidazo[1,5-A][ 1,4]Benzodiazepine-3-Carboxylate

上下游产品

(3-(ethoxycarbonyl)-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepin-8-yl)(4-methylphenyl)iodonium tosylate (3-(ethoxycarbonyl)-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepin-8-yl)(phenyl)iodonium tosylate (3-(ethoxycarbonyl)-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepin-8-yl)(2-thiophenyl)iodonium tosylate (3-(ethoxycarbonyl)-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepin-8-yl)(3-thiophenyl)iodonium tosylate

4-甲基-3,4-二氢-1H-苯并[e][1,4]二氮杂卓-2,5-二酮置于sodium Hydride体系中,化学反应 1.58H,反应生成 氟马西尼杂质
参考文献:咪唑并[1,5-A] [1,4]苯并二氮杂s酯在"对地西p不敏感"的苯并二氮杂receptor受体上具有高亲和力和选择性的合成和评价.
标题:咪唑并[1,5-A] [1,4]苯并二氮杂s酯在"对地西p不敏感"的苯并二氮杂receptor受体上具有高亲和力和选择性的合成和评价.
摘要:已经合成了具有不同酯侧链和8位取代基的一系列咪唑并[1,5-A] [1,4]苯并二氮杂酸酯.在苯二氮卓受体(bzr)的"对地西ze不敏感"(di)和对地西epa敏感(ds)的亚型下评估了这些化合物的亲和力.观测到3-位酯侧链部分对di处的配体亲和力具有深远的空间效应.相反,酯的大小对ds上的配体亲和力影响较小.在一系列的8-氯酯中,叔丁基酯化合物8对di表现出最高的亲和力(ki = 1.7 Nm).此外,在所检查的一系列叔丁酯中,在8位上的卤素导致配体亲和力和di选择性的提高.8-硝基衍生物23和8-异硫氰酸根同源物25对di和ds均具有高亲和力,但几乎没有亚型选择性(di分别为10.8和2.7 Nm,Ds分别为14和3.7 Nm).8-叠氮基叔丁酯29显示出比相应的乙酯,原型di配体1(ro 15-4513)明显更高的亲和力(ki = 0.43 Nm)和选择性(di / Ds比为0.2)
DOI:10.1021/jm00060A007

专利信息

专利号:US-8895727-B2
优先权日:2011-05-25
标题 :Method for preparation of fluorine-18-labeled flumazenil using diaryliodonium salt precursor
发明人：LEE BYUNG CHUL; MOON BYUNG SEOK; KIM JI SUN
权利人:BIO IMAGING KOREA CO LTD
摘要:Disclosed is the synthesis of [ 18 F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [ 18 F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [ 18 F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix 2.2.2. /potassium carbonate(K 2.2.2. /K 2 CO 3 ) and TEMPO in dimethylformamide (DMF) at a high yield.