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Synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile: a key intermediate for dipeptidyl peptidase IV inhibitors.
Beilstein Journal of Organic Chemistry ( IF 2.2 ) Pub Date : 2008 , DOI: 10.3762/bjoc.4.20
Santosh Kumar Singh , Narendra Manne , Manojit Pal

An alternative and practical synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile was achieved. Reaction of L-proline with chloroacetyl chloride was followed by conversion of the carboxylic acid moiety of the resulting N-acylated product into the carbonitrile via the corresponding amide intermediate. The synthesized pyrrolidine derivative was utilized to prepare DPP-IV inhibitor Vildagliptin.

中文翻译:

(S)-1-(2-氯乙酰基)吡咯烷-2-腈的合成:二肽基肽酶IV抑制剂的关键中间体。

(S)-1-(2-氯乙酰基)吡咯烷-2-腈的另一种实用合成方法。使L-脯氨酸与氯乙酰氯反应,然后将所得N-酰化产物的羧酸部分通过相应的酰胺中间体转化为腈。合成的吡咯烷衍生物用于制备DPP-IV抑制剂维格列汀。
更新日期:2017-01-31
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