CAS: 3551-55-1; 2,4-Dimethoxypyrimidine

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13106-85-9 29458-38-6 7781-23-9

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5-氯-2,4-二甲氧基嘧啶置于[1,3-Bis[2,6-Bis[3-Methyl-1-(2-Methylpropyl)Butyl]Phenyl]-4,5-Dichloro-1,3-Dihydro-2H-Imidazol-2-Ylidene]Chloro[(1,2,3-η)-1-Phenyl-2-Propen-1-Yl]Palladium,Sodium 2,6-Di-Tert-Butyl-4-Methylphenoxide体系中,用 四氢呋喃 用作溶剂,化学反应 24.0H,以85%的收率获得2,4-二甲氧基嘧啶
参考文献:丁酸钠羟基甲苯(nabht)作为pd催化还原反应的新型高效氢化物来源.
标题:丁酸钠羟基甲苯(nabht)作为pd催化还原反应的新型高效氢化物来源.
摘要:Nabht(丁基羟基甲苯钠),一种受阻且可溶的碱,用于各种碱敏性胺和(杂)芳基卤化物的有效芳基化,已发现其作为氢化物供体的作用是出乎意料的,以减少(杂)芳基卤化物和乙酸烯丙酯.机理研究发现,Nabht而非bht可以通过将nabht中的苄基甲基氧化为醛来递送多种氢化物.此外,用nabht-D20进行还原已经表明,氧化还原活性苄基位置不是来自nabht的唯一氢化物供体位点,其中三分之一的氢化物可能来自叔丁基.在温和的条件下,还原效果很好,而且令人难以置信的是,在此过程中仅消耗了20%的nabht.其余的80%可以很容易地以纯净的形式回收再利用.这,
Doi:10.1002/chem.201902876

专利信息

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:WO-2007141253-A1
优先权日:2006-06-07
标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines
发明人：PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO
摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:US-11542234-B2
优先权日:2018-03-16
标题 :2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues
发明人：NEUMAIER BERND; ZLATOPOLSKIY BORIS; KRAPF PHILIPP; RICHARZ RAPHAEL; DRZEZGA ALEXANDER
权利人:UNIV KOELN
摘要:6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the 18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

专利号:US-12304912-B2
优先权日:2020-07-28
标 题 :Fused bicyclic RAF inhibitors and methods for use thereof
发明人：BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA
权利人:JAZZ PHARMACEUTICALS IRELAND LTD
摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.

专利号:CN-1187339-C
优先权日:1998-07-23
标 题:Process for the preparation of 4,6-disubstituted 2-isocyanatopyrimidines and their use as intermediates in the synthesis of active compounds

专利号:CN-1311782-A
优先权日:1998-07-23
标 题:Process for the preparation of 4,6-disubstituted 2-isocyanatopyridines and their use as intermediates in the synthesis of active compounds