如何制备5-氟-2-甲基苯基溴化镁格氏试剂? 5-氟-2-甲基苯基溴化镁是一种常用的医药合成中间体。 制备方法 通过在单一CSTR中生成格氏试剂来制备5-氟-2-甲基苯基溴化镁。首先,在MeTHF(1L)中活化镁(227g,9.4mol)浆液,制备1.0MINT1格氏试剂(1207g)。然后,将化合物1(23%(w/w))以34.5mL/min的速度加入CSTR中,反应溶液通过汲取管离开,用作隔离CSTR中的固体镁。最后,将溶液以1倍的速率收集在积聚容器中。该操作运行超过5天,总处理时间为32小时。5-氟-2-甲基苯基溴化镁产量为1.68千克(69.6摩尔),转化率为97%,收率为95%。 应用 5-氟-2-甲基苯基溴化镁可以参与多种反应。 可以通过连续泵送5-氟-2-甲基苯基溴化镁格氏试剂(1.02M)和DMF(10%(w/w))混合物,加入4MLiBH4,然后将溶液连续泵入CSTR2中。在操作0.5小时后,加入甲醇和H2SO4,浓度为15.1mL/分钟。最后,加入甲苯,合并有几层,用NaHCO3水溶液洗涤,将浓缩至油状物。通过过滤和干燥,可以得到555g化合物2,纯度为99.9%。 主要参考资料 [1] FlowGrignardandLithiation:Screening Toolsand Development of Continuous Processes for a BenzylAlcoholStartingMaterial 查看更多
人胃粘膜上皮细胞提取物的应用及其研究意义? 人胃粘膜上皮细胞提取物是从人原代胃粘膜上皮细胞提取的,可用于基因克隆、表达图谱分析以及各种分子生物学实验的研究。上皮细胞覆盖于身体表面并衬贴于体内空腔器官腔面的细胞,具有保护、吸收、分泌和排泄等作用。胃粘膜是胃壁的最内层,胃粘膜上皮细胞主要功能是分泌胃酸、各种消化酶,并分泌黏液覆盖于胃黏膜的表面,防止胃酸和胃蛋白酶对胃黏膜的损害。 人胃粘膜上皮细胞失巢凋亡及其机制研究的意义 失巢凋亡是指细胞脱离粘附后发生的程序化细胞死亡,而胃癌细胞具有抵抗失巢凋亡的能力,从而导致其通过血液和淋巴转移至远处器官进行异位定植。然而,胃癌细胞发生失巢凋亡抵抗的分子机制还不清楚。SFRP1是一种在胃癌等多种恶性肿瘤组织中低表达或表达缺失的蛋白质。通过沉默GES-1细胞中SFRP1表达,可以研究SFRP1对胃粘膜上皮细胞失巢凋亡敏感性的影响,并进一步探讨SFRP1调控胃粘膜上皮细胞失巢凋亡的分子机制,为研究SFRP1在胃癌发展中的作用及机制提供新的思路和理论依据。 参考文献 [1] Anoikis resistant human osteosarcoma cells display significant angiogenesis by activating the Src kinase mediated MAPK pathway[J]. Ziran Gao, Guo Sheng Zhao, Yangfan Lv, Dongbin Peng, Xuefeng Tang, Hanxiang Song, Qiao Nan Guo. Oncology Reports. 2019(1) [2] Inhibin B suppresses anoikis resistance and migration through the transforming growth factor‐β signaling pathway in nasopharyngeal carcinoma[J]. Guoying Zou, Biqiong Ren, Yi Liu, Yin Fu, Pan Chen, Xiayu Li, Shudi Luo, Junyu He, Ge Gao, Zhaoyang Zeng, Wei Xiong, Guiyuan Li, Yumei Huang, Keqian Xu, Wenling Zhang. Cancer Science. 2018(11) [3] Targeting the Wnt/beta-catenin pathway in cancer: Update on effectors and inhibitors[J]. Nithya Krishnamurthy, Razelle Kurzrock. Cancer Treatment Reviews. 2018 [4] Downregulation of Bit1 expression promotes growth, anoikis resistance, and transformation of immortalized human bronchial epithelial cells via Erk activation-dependent suppression of E-cadherin[J]. Xin Yao, Selena Gray, Tri Pham, Mychael Delgardo, An Nguyen, Stephen Do, Shubha Kale Ireland, Renwei Chen, Asim B. Abdel-Mageed, Hector Biliran. Biochemical and Biophysical Research Communicatio. 2018(1) [5] Epithelial–mesenchymal transition (EMT): A biological process in the development, stem cell differentiation, and tumorigenesis[J]. Tong Chen, Yanan You, Hua Jiang, Zack Z. Wang. Journal of Cellular Physiology. 2017(12) [6] Targeting of Aberrant αvβ6 Integrin Expression in Solid Tumors Using Chimeric Antigen Receptor-Engineered T Cells[J]. Lynsey M. Whilding, Ana C. Parente-Pereira, Tomasz Zabinski, David M. Davies, Roseanna M. G. Petrovic, Y. Vincent Kao, Shobhit A. Saxena, Alex Romain, Jose A. Costa-Guerra, Shelia Violette, Hiroaki Itamochi, Sadaf Ghaem-Maghami, Sabari Vallath, John F. Marshall, John Maher. Molecular Therapy. 2017(1) [7] Tight Sequestration of BH3 Proteins by BCL-xL at Subcellular Membranes Contributes to Apoptotic Resistance[J]. Jessie Pécot, Laurent Maillet, Janic Le Pen, Céline Vuillier, Sophie de Carné Trécesson, Aurélie Fétiveau, Kristopher A. Sarosiek, Florian J. Bock, Frédérique Braun, Anthony Letai, Stephen W. G. Tait, Fabien Gautier, Philippe P. Juin. Cell Reports. 2016(12) [8] 汤晓琳. SFRP1基因沉默抑制人胃粘膜上皮细胞失巢凋亡及其机制研究[D]. 沈阳医学院, 2019. 查看更多