Dana Grunhaus,Estefanía Rossich Molina,Roni Cohen et al.
Dana Grunhaus et al.
Preparing phosphorylated peptides with multiple adjacent phosphorylations is synthetically difficult, leads to β-elimination, results in low yields, and is extremely slow. We combined synthetic chemical methodologies with computational stu...
Synthesis of MDM2-p53 Inhibitor BI-0282 via a Dipolar Cycloaddition and Late-Stage Davis-Beirut Reaction [0.03%]
BI-0282的合成——通过双极性环加成及后期戴维斯-贝鲁特反应抑制MDM2-p53蛋白质相互作用
Juergen Ramharter,Michael Kulhanek,Maike Dettling et al.
Juergen Ramharter et al.
Herein, we report the structure and synthesis of the potent MDM2-p53 inhibitor BI-0282. The complex spirooxindole scaffold bearing four stereocenters embedded in a rigid polycyclic ring-system was effectively prepared on a multi-gram scale ...
High-Yield Synthesis of Enantiopure 1,2-Amino Alcohols from l-Phenylalanine via Linear and Divergent Enzymatic Cascades [0.03%]
以L-苯丙氨酸为原料高效合成单一对映体的1,2-氨基醇：线性及发散式联酶催化串联反应体系的研究
Maria L Corrado,Tanja Knaus,Ulrich Schwaneberg et al.
Maria L Corrado et al.
Enantiomerically pure 1,2-amino alcohols are important compounds due to their biological activities and wide applications in chemical synthesis. In this work, we present two multienzyme pathways for the conversion of l-phenylalanine into ei...
Synthesis of Enantiopure Unnatural Amino Acids by Metallaphotoredox Catalysis [0.03%]
手性纯非天然氨基酸的金属光氧化还原催化合成法
Tomer M Faraggi,Caroline Rouget-Virbel,Juan A Rincón et al.
Tomer M Faraggi et al.
We describe herein a two-step process for the conversion of serine to a wide array of optically pure unnatural amino acids. This method utilizes a photocatalytic cross-electrophile coupling between a bromoalkyl intermediate and a diverse se...
Design, Development, and Analysis of an Automated Sampling Loop for Online Monitoring of Chiral Crystallization [0.03%]
用于在线手性结晶监测的自动取样回路的设计、开发和分析
Ghufran Ur Rehman,Thomas Vetter,Philip A Martin
Ghufran Ur Rehman
Enantiomeric purity is of prime importance for several industries, specifically in the production of pharmaceuticals. Crystallization processes can be used to obtain pure enantiomers in a suitable solid form. However, some process variants ...
Marcos Veguillas Hernando,Jonathan C Moore,Rowena A Howie et al.
Marcos Veguillas Hernando et al.
A new continuous-flow process is presented for synthesis of the pharmaceutical intermediate norketamine (5). Our approach has been to take the well-established and industrially applied batch synthetic route to this promising antidepressant ...
Binary Solvent Swap Processing in a Bubble Column in Batch and Continuous Modes [0.03%]
批次和连续模式下气泡柱中的二元溶剂交换过程
Phillip Roche,Roderick C Jones,Brian Glennon et al.
Phillip Roche et al.
A lab-scale bubble column was investigated as an alternative means to achieve a low-temperature binary solvent swap of solutions containing pharmaceutical materials at atmospheric pressure, for batch and continuous configurations. The rate ...
Scale-Up of a Heterogeneous Photocatalytic Degradation Using a Photochemical Rotor-Stator Spinning Disk Reactor [0.03%]
基于光化学旋转型盘式反应器的多相光催化降解放大研究
Arnab Chaudhuri,Stefan D A Zondag,Jasper H A Schuurmans et al.
Arnab Chaudhuri et al.
Many chemical reactions contain heterogeneous reagents, products, byproducts, or catalysts, making their transposition from batch to continuous-flow processing challenging. Herein, we report the use of a photochemical rotor-stator spinning ...
Scalable Flow Electrochemical Alcohol Oxidation: Maintaining High Stereochemical Fidelity in the Synthesis of Levetiracetam [0.03%]
可扩展流电化学氧化酒精反应：在左乙拉西坦合成中保持高立体化学保真度
Xing Zhong,Md Asmaul Hoque,Matthew D Graaf et al.
Xing Zhong et al.
An electrochemical flow process has been developed for an alcohol oxidation step in the synthesis of the generic epilepsy drug levetiracetam. A crucial metric in this process is the retention of high enantiomeric purity as the oxidation of ...
A New Scalable Synthesis of ELQ-300, ELQ-316, and other Antiparasitic Quinolones [0.03%]
一种新型可扩展合成ELQ-300、ELQ-316及其他抗寄生虫喹诺酮类药物的方法
Sovitj Pou,Rozalia A Dodean,Lisa Frueh et al.
Sovitj Pou et al.
The Endochin-Like Quinolone (ELQ) compound class may yield effective, safe treatments for a range of important human and animal afflictions. However, to access the public health potential of this compound series, a synthetic route needed to...