维格列汀中间体的高效合成

IF 0.5 4区化学 Q3 Pharmacology, Toxicology and Pharmaceutics

Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry Pub Date : 2021-10-07 DOI:10.56042/ijcb.v60i8.30478

Yufei Li, Lan Jiang, Li Zhang, Jingyu Wang, Peng Xiang, J. Pan, Xiangnan Hu

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引用次数: 0

摘要

介绍了制备维格列汀1中间体(S)-1-(2-氯乙酰基)吡咯烷-2-碳腈2和3-氨基-1-金刚烷醇3的高效高产方法。以l -脯氨酸2a为原料，以氯乙酰为原料，在硫酸存在下与乙腈进行一锅反应，合成了(S)-1-(2-氯乙酰基)吡咯烷-2-碳腈2。以盐酸金刚烷胺为原料，以硫酸/硝酸、硼酸为催化剂氧化制得3-氨基-1-金刚烷醇3，并进行乙醇萃取。总收率约为95%。

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An efficient synthesis of Vildagliptin intermediates

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%.

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来源期刊

Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry 化学-有机化学

自引率

0.00%

发文量

审稿时长

4-8 weeks

期刊介绍： Indian Journal of Chemistry (Section B) is a leading monthly journal in Organic and Medicinal Chemistry started publishing from 1976. It publishes papers on organic reaction mechanism, theoretical organic chemistry, structure-activity relationships, medicinal chemistry, synthesis of chiral compounds, bio-organic chemistry, enzymes in organic synthesis, reagents in organic synthesis, heterocyclic compounds, phytochemistry (natural products), amino acids, peptides and proteins, spectroscopy in characterization of organic compounds, chemoenzymatic and enantioselective synthesis of organic compounds, synthesis of fullerenes, metal-catalyzed asymmetric reactions, bioactive plant products and combinatorial chemistry. Apart from full length papers, notes and communications, the journal publishes short reviews on frontline areas under the column " advances in Contemporary Research".