Diabetes is on the rise across the Globe and millions of people are being affected. Sitagliptin has emerged as a potent inhibitor for the treatment of type II diabetes, which can regulate blood sugar level, and new strategies to prepare this molecule are being discovered. Herein we report a highly enantioselective synthesis of sitagliptin. Using specifically identified chiral FerroLANE ligands in the presence of a rhodium catalyst the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee). The final product has been isolated as a phosphate salt with >99% ee. More information can be found in the Full Paper by Samir Chikkali et al.

中文翻译：

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西他列汀的高度对映选择性合成

糖尿病在全球范围内呈上升趋势，数百万人受到影响。西他列汀已成为治疗II型糖尿病的有效抑制剂，可调节血糖水平，并且正在发现制备该分子的新策略。在本文中，我们报道了西他列汀的高度对映选择性合成。在铑催化剂的存在下，使用经过特别鉴定的手性FerroLANE配体，烯胺的不对称氢化生成西他列汀，具有出色的对映选择性（98％ee）。最终产物已分离为ee > 99％的磷酸盐。可以在Samir Chikkali等人的《全文》中找到更多信息。