Efficient and high yielding methods for the preparation of vildagliptin 1 intermediate of (S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile 2 and 3-amino-1-adamantane alcohol 3 respectively have been described. (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 2 has been synthesized from L-proline 2a via chloroacetyl chloride, performed with acetonitrile in the presence of sulfuric acid via one-pot reactions. 3-Amino-1-adamantane alcohol 3 has been prepared from amantadine hydrochloride via oxidation by sulfuric acid/nitric acid and boric acid as catalyst, and has been subjected to ethanol extraction. The overall yield is about 95%.

中文翻译：

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维格列汀中间体的高效合成

已经描述了分别用于制备(S)-1-(2-氯乙酰基)吡咯烷-2-甲腈2和3-氨基-1-金刚烷醇3的维格列汀1中间体的高效且高产的方法。(S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 2 已由 L-脯氨酸 2a 通过氯乙酰氯合成，在硫酸存在下用乙腈通过一锅反应进行。3-氨基-1-金刚烷醇3是以盐酸金刚烷胺为原料，以硫酸/硝酸和硼酸为催化剂，经氧化反应制备得到3-氨基-1-金刚烷醇3，并经乙醇提取。总收率约为95%。