两步法合成(S)-1-(2-氯乙酰基)-2-腈基吡咯烷的工艺研究

目的 研究(S)-1-(2-氯乙酰基)-2-腈基吡咯烷的合成工艺.方法 L-脯氨酸与氯乙酰氯通过N-乙酰化得到(S)-1-(2-氯乙酰基)-2-吡咯烷甲酸,然后加入脲素和氨基磺酸实行分段保温反应得到产物(S)-1-(2-氯乙酰基)-2-腈基吡咯烷.结果 此路线所得产品收率为75.5％.结论 此工艺路线条件温和、操作简便、原料价廉易得.

Technology of two-step synthesis for (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile

Objective To study the synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile. Methods L-Proline was N-acylated with chloroacetyl chloride to prepare (S)-1-(2-chloroacetyl)pyrrolidine-2-carboxylic acid, then urea and sulfamic acid were added, and (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile was given by using segmented insulation. Results The yield of (S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile was 75.5%. Conclusion The reaction conditions of this route are mild, operation is easy, and the materials are common and inexpensive.