Nelarabine is a prodrug of the deoxyguanosine analogue, 9-β-D-arabinofuranose guanine (ara-G), which is used for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). For the clinical study of nelarabine and its active ingredient, ara-G, a suitable isotope-labeled internal standard was required. Effective and operationally simple methods for the synthesis of [D 4 ]]nelarabine and [D 3 ]ara-G were developed with high deuterium incorporation using D 2 O, CD 3 OD and NaBD 4 as deuterium sources. It was found that [D 3 ]ara-G was useful as an internal standard instead of [D 4 ]nelarabine. Graphic abstract Nelarabine is a prodrug of the deoxyguanosine analogue, 9-β-D-arabinofurose guanine (ara-G), which is used for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). For the clinical study of nelarabine and its active ingredient, ara-G, a suitable isotope-labeled internal was not suitable as an internalstandard was required. Effective and operationally simple methods for the synthesis of [D 4 ]]nelarabine and [D 3 ]ara-G were developed with high deuterium incorporation using D 2 O, CD 3 OD and NaBD 4 as deuterium sources. It was found that [D 3 ]ara-G was useful as an internal standard instead of [D 4 ]nelarabine.

中文翻译：

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氘标记奈拉滨及其活性成分ara-G的合成

奈拉滨是脱氧鸟苷类似物 9-β-D-阿拉伯呋喃糖鸟嘌呤 (ara-G) 的前药，用于治疗 T 细胞急性淋巴细胞白血病 (T-ALL) 和 T 细胞淋巴母细胞淋巴瘤。 T-LBL）。对于奈拉滨及其活性成分 ara-G 的临床研究，需要合适的同位素标记内标。使用 D 2 O、CD 3 OD 和 NaBD 4 作为氘源，开发了合成 [D 4 ]]奈拉滨和 [D 3 ]ara-G 的有效且操作简单的方法，其中氘掺入率高。发现[D 3 ]ara-G代替[D 4 ]奈拉滨可用作内标。图形摘要奈拉滨是脱氧鸟苷类似物 9-β-D-阿拉伯呋喃鸟嘌呤 (ara-G) 的前药，用于治疗 T 细胞急性淋巴细胞白血病 (T-ALL) 和 T 细胞淋巴细胞淋巴瘤 (T-LBL) 患者。对于奈拉滨及其活性成分 ara-G 的临床研究，由于需要合适的同位素标记内标，因此不合适。使用 D 2 O、CD 3 OD 和 NaBD 4 作为氘源，开发了合成 [D 4 ]]奈拉滨和 [D 3 ]ara-G 的有效且操作简单的方法，其中氘掺入率高。发现[D 3 ]ara-G代替[D 4 ]奈拉滨可用作内标。使用 D 2 O、CD 3 OD 和 NaBD 4 作为氘源，开发了合成 [D 4 ]]奈拉滨和 [D 3 ]ara-G 的有效且操作简单的方法，其中氘掺入率高。发现[D 3 ]ara-G代替[D 4 ]奈拉滨可用作内标。使用 D 2 O、CD 3 OD 和 NaBD 4 作为氘源，开发了合成 [D 4 ]]奈拉滨和 [D 3 ]ara-G 的有效且操作简单的方法，其中氘掺入率高。发现[D 3 ]ara-G代替[D 4 ]奈拉滨可用作内标。