D-脯氨酰胺的合成新工艺  

New synthetic route for D-prolinamide

作　　者：王蓓[1] 许文松[1] 栗更新[1] 徐六兴[1] 

机构地区：[1]浙江大学材料与化工学院制药工程研究所,浙江杭州310027

出　　处：《中国药物化学杂志》2005年第5期285-287,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的研究手性中间体D-脯氨酰胺合成的新工艺。方法以L-脯氨酸为起始原料,S-酒石酸为拆分剂,运用不对称转换的方法合成D-脯氨酸。进一步应用手性源技术,经氨基保护、酯化、氨化和脱保护等步骤,不对称合成目标化合物。结果与结论目标化合物收率达到78.4%,光学纯度达到99.3%(以D-脯氨酸计)。新工艺与专利文献相比,具有收率高,光学纯度好的特点,更适合工业化生产。Aim To establish a new method for the synthesis of D-prolinamide. Method D-proline was obtained from the asymmetric transformafion of L-proline via the formation of （ S）-tartaric acid salt by using butanal as catalyst. Then, D-prolinamide was synthesized by amino protection, esterification, amidation and deprotection. Results and conclusion The yield of final product was 78.4 % and optical purity was 99.3 %. Comparing with patent synthetic procedure for D-prolinamide, it is a new synthetic procedure with better yield and purity and suitable for industrial manufacture.

关 键 词：药物化学 工艺改进 不对称合成 手性药物 D-脯氨酰胺 

分 类 号：TQ463[化学工程—制药化工]