重氢（2 H）磁共振成像是一种新兴方法，可非侵入性地研究体内葡萄糖代谢，对于理解病因和监测诸如肿瘤、糖尿病和神经退行性疾病等许多疾病的进展非常重要。然而，2 H标记葡萄糖的合成成本昂贵，因为原材料昂贵且需要极端反应条件，使得2 H标记的葡萄糖相当昂贵且难以承受临床使用。在本研究中，我们提出一种新的重氘化合物-[2,3,4,6,6'-2 H5 ]-D-葡萄糖，其生产成本降低约10倍。合成路线使用更便宜的原材料甲基-α-D-葡萄糖苷，依赖于温和的反应条件（80°C），并具有更高的重氘标记效率。磁共振光谱（MRS）和质谱实验证实化合物的成功重氘标记。动物研究证明，通过超高场系统上的2 H-MRS定量下游代谢产物，该底物可描述胶质瘤大鼠模型的糖酵解代谢。在动物研究中，对比了[2,3,4,6,6'-2 H5 ]-D-葡萄糖和商业[6,6'-2 H2 ]-D-葡萄糖的葡萄糖代谢特性。这种成本效益的化合物将有助于促进重氢磁共振成像的临床转化，并使这种强大的代谢成像模态广泛应用于基础研究和临床应用。©2022 John Wiley & Sons Ltd.

Deuterium (2 H) magnetic resonance imaging is an emerging approach for noninvasively studying glucose metabolism in vivo, which is important for understanding pathogenesis and monitoring the progression of many diseases such as tumors, diabetes, and neurodegenerative diseases. However, the synthesis of 2 H-labeled glucose is costly because of the expensive raw substrates and the requirement for extreme reaction conditions, making the 2 H-labeled glucose rather expensive and unaffordable for clinic use. In this study, we present a new deuterated compound, [2,3,4,6,6'-2 H5 ]-D-glucose, with an approximate 10-fold reduction in production costs. The synthesis route uses cheaper raw substrate methyl-α-D-glucopyranoside, relies on mild reaction conditions (80°C), and has higher deuterium labeling efficiency. Magnetic resonance spectroscopy (MRS) and mass spectroscopy experiments confirmed the successful deuterium labeling in the compound. Animal studies demonstrated that the substrate could describe the glycolytic metabolism in a glioma rat model by quantifying the downstream metabolites through 2 H-MRS on an ultrahigh field system. Comparison of the glucose metabolism characteristics was carried out between [2,3,4,6,6'-2 H5 ]-D-glucose and commercial [6,6'-2 H2 ]-D-glucose in the animal studies. This cost-effective compound will help facilitate the clinical translation of deuterium magnetic resonance imaging, and enable this powerful metabolic imaging modality to be widely used in both preclinical and clinical research and applications.© 2022 John Wiley & Sons Ltd.