Simplified Labeling Approach for Synthesizing 3′-Deoxy-3′-[18F]fluorothymidine ([18F]FLT)

[¹⁸F]FLT (3-deoxy-3-[¹⁸F]fluorothymidine) turned out to be a tracer particularly suitable for PET imaging of tumor proliferation because of lacking degradation in vivo. To facilitate clinical studies with [¹⁸F]FLT, we investigated two new easily accessible precursors, 2,3-anhydrothymidine (AThy) and 5-O-(4,4-dimethoxytriphenylmethyl)-2,3-anhydrothymidine (DMTThy), using a common approach for introducing the label with nucleophilic [¹⁸F]fluoride. Radiochemical yields were determined in dependence on substrate concentration, reaction time and temperature. In the case of AThy (10 mg), best FLT yields were 5.3%±1.2 (130 °C, 30 min). Labeling of DMTThy (10 mg) gave 14.3%±3.3 at 160 °C within 10 minutes. Starting with an aqueous solution of 20 GBq [¹⁸F]fluoride the new method allows to produce 1.3 GBq [¹⁸F]FLT within 90 minutes ready for intravenous injection. The new labeling procedures allow [¹⁸F]FLT synthesis without lengthy preparation of the precursor and with high reproducibility mandatory for clinical application.     

Synthesis of fluorinated imines and carbodiimides from azides via aza-Wittig reaction

The Staudinger reaction of fluoroalkylazides were studied. A series of N-fluoroalkylimines were synthesized via aza-Wittig reaction of N-fluoroalkyliminophosphoranes. The N,N′-difluoroalkylated carbodiimide was also synthesized via the reaction of N-fluoroalkyliminophosphoranes with carbon dioxide or carbon disulfide.     

Mass resolved MPI spectra of methyl iodide in the 430-490 nm region

The mass resolved multiphoton ionization (MPI) spectra of methyl iodide were obtained in the 430-490 nm region using a time-of-flight (TOF) mass spectrometer. They have the same vibrational structure, which testifies that the fragment species, in the wavelength region under study, are from the photodissociation of multiphoton ionized molecular parent ions. Some features in the spectra are identified as three-photon excitations to 6p and 7s Rydberg states of methyl iodide. Two new vibrational structures of some Rydberg states are observed. The mechanism of ionization and dissociation is also discussed.     

A new synthesis of 1,2,3,5‐tetrahydroimidazo[2,3‐b]‐[1,3]benzodiazocines

A new synthesis of 6‐carbomethoxy‐1,2,3,5‐tetrahydroirnidazo[2,3‐b][1,3]benzodiazocines 13 by the intramolecular cycloaddition reaction of methyl 2‐(1‐aziridinylmethyl)‐3‐(2‐ureidophenyl)propenoates 10 under Appel's dehydration conditions is described. The latter were readily obtained from 2‐nitrobenzalde‐hyde with methyl acrylate through the Baylis‐Hillman reaction.     

聚合物在碳纤维表面的电沉积

用电沉积方法将苯乙烯-马来酸酐、乙酸乙烯酯-马来酸酐、甲基丙烯酸甲酯-马来酸酐共聚物沉积于碳纤维表面。通过实验初步证实了此过程的负离子-自由基机理,以及沉积层在纤维表面的物理粘附。由于电沉积的聚合物中间层改善了碳纤维增强塑料中纤维-基体树脂间的界面粘接作用,使原来的剪切破坏基本上发生于界面的情况转变成发生于基体本身为主。并将单向碳纤维增强环氧树脂复合材料的层间剪切强度,由原来的600kg/cm~2左右提高到1000kg/cm~2以上,经沸水浸泡100小时后的强度损失也减少了。     

14‐Membered Cyclopeptides from Paliurus ramosissimus and P. hemsleyanus

Six 14‐membered cyclopeptide alkaloids, i.e., ramosines A–C, mucronine J, and lotusines A and D, were isolated from the roots of Paliurus ramosissimus, and an additional four, hemsines A–D, from the roots of P. hemsleyanus. Among these, ramosines A–C ( 1, 5 , and 6 , resp.) and hemsines A and B ( 7 and 8 , resp.) are new bases of the amphibine‐B type, and hemsines C and D ( 9 and 10 , resp.) are new integerrine‐type alkaloids. Additionally, ramosine C ( 6 ) represents the first 14‐membered cyclopeptide alkaloid possessing a substitution (? OH) at C(13′). Their structural elucidations were based on spectral analysis and molecular‐modeling studies. Pronounced solvent effects in the ¹H‐ and ¹³C‐NMR spectra of these two types of alkaloids were observed.