In this paper, N-(2-[18F]fluoropropionyl)-β-glutamic acid 8 ([18F]FP-β-Glu), a new N-substituted 18F-labeled amino acid tracer, was synthesized from the precursor 4 (diethyl 3-(2-bromopropanamido)pentanedioate) via a two-step reaction on the modified FDG synthesizer. The radiochemical yield was 20 ± 5% (n = 10, decay-corrected) from [18F]fluoride within 40 min, the radiochemical purity was 98%. Moreover, microPET studies showed that [18F]FP-β-Glu 8 exhibited rapid tumor uptake and good tumor-to-lung ratio in SPC-A-1 tumor-bearing mice. A high accumulation of radioactivity was found in the kidneys and bladder, which suggested that the tracer was mainly eliminated through the urinary system.

A Lewis acid catalyzed intramolecular [3 + 2] cross cycloaddition of cobalt-alkynylcyclopropane 1,1-diesters with carbonyls has been successfully developed. Together with simple and efficient postcycloadditions of the cobalt-alkyne moiety, a general and efficient strategy for construction of structurally complex and diverse medium-sized skeletons and related polycycles was supplied successfully.

The noninvasive imaging of cell death, including apoptosis and necrosis, is an important tool for the assessment of degenerative diseases and in the monitoring of tumor treatments. Duramycin is a peptide of 19-amino acids. It binds specifically to phosphatidylethanolamine a novel molecular target for cell death. N-(2-18F-Fluoropropionyl)duramycin ([18F]FPDuramycin) was prepared as a novel positron emission tomography (PET) tracer from the reaction of duramycin with 4-nitrophenyl 2-[18F]fluoropropionate ([18F]NFP). Compared with control cells (viable tumor cells), the in vitro binding of [18F]FPDuramycin with apoptotic cells induced by anti-Fas antibody resulted in a doubling increase, while the binding of [18F]FPDuramycin with necrotic cells induced by three freeze and thaw cycles resulted in a threefold increase. Biodistribution study in mice exhibited its rapid blood and renal clearance and predominant accumulation in liver and spleen over 120 min postinjection. Small-animal PET/CT imaging with [18F]FPDuramycin proved to be a successful way to visualize in vivo therapeutic-induced tumor cell death. In summary, [18F]FPDuramycin seems to be a potential PET probe candidate for noninvasive visualization of in vivo cell death sites induced by chemotherapy in tumors.

A mild and convenient transformation for the synthesis of nitro-polyols is described. The nitro-polyol derivatives were prepared either from 2-nitroglycals via a pyridine-promoted scission of the carbon–carbon double bond or from glycals via a sequential nitration–scission procedure. The generated nitro-polyols could undergo a stereoselective Michael addition reaction. The utility of the addition products was exemplified by the concise synthesis of (−)-hyacinthacine A1 and 7a-epi-(−)-hyacinthacine A1.