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Jiang G.-Y.,Hebei University of Science and Technology | Zhang Y.,Hebei University of Science and Technology | Zhang Y.,State Key Laboratory Breeding Base Key Laboratory of Molecular Chemistry for Drug of Hebei Province | Cao W.-T.,Hebei University of Science and Technology
Chinese Journal of New Drugs | Year: 2016

Objective: To synthesize DBPR108 (1), a dipeptidyl peptidase IV inhibitor. Methods: Started from 4-methylpent-3-en-2-one (2), the key intermediate 3-amino-3-methyl-1-(pyrrolidin-1-yl) butan-1-one hydrochloride (7) was obtained by addition, protection, haloform reaction, amidation and deprotection reaction, and then condensed with (2S, 4S)-1-(2-chloroacetyl)-4-fluoropyrrolidine-2-carbonitrile (8) to get the target compound 1. Results: The structure of DBPR108 was confirmed by 1H NMR, 13C NMR and ESI-MS. The overall yield was 16%, and the product purity was up to 99.5%. Conclusion: This synthetic process needs mild reaction condition, which is easy to operate with high yield.


Wang W.,Hebei University of Science and Technology | Yang J.-L.,Hebei University of Science and Technology | Zhang Y.,Hebei University of Science and Technology | Zhang Y.,State Key Laboratory Breeding Base Key Laboratory of Molecular Chemistry for Drug of Hebei Province
Chinese Journal of New Drugs | Year: 2014

Objective: To improve the synthesis process of retigabine. Methods: The target compound was synthesized from 3-fluoroaniline by acetylation and nitrification to give N-(5-fluoro-2-nitrophenyl)acetamide (2), which was subjected to condensation with (4-fluorophenyl) methanamine to afford N-(5-((4-fluorobenzyl)amino)-2-nitrophenyl) acetamide (3), followed by deacetylation, reduction, and acylation. Results: The structure of retigabine was confirmed by 1H-NMR and MS. The overall yield was 39.6%. Conclusion: This synthetic process is easy to scale up for its convenient operation.


Zhao L.,Hebei University of Science and Technology | Fan S.-S.,Hebei University of Science and Technology | Zhang Y.,Hebei University of Science and Technology | Zhang Y.,State Key Laboratory Breeding Base Key Laboratory of Molecular Chemistry for Drug of Hebei Province
Chinese Journal of New Drugs | Year: 2014

Objective: To synthesize melogliptin, a dipeptidyl peptidase IV inhibitor, and optimize the preparation process.Methods: The target compound was synthesized from (±)-2-azabicyclo[2, 2, 1]hept-5-en-3-one (2) by ten steps including protection, reduction and condensation.Results: The structure of melogliptin was confirmed by 1H-NMR, 13C-NMR and ESI-MS. The overall yield was 13%.Conclusion: This synthetic process needs mild reaction condition, which is easy to operate with high yield. ©, 2014, Chinese Journal of New Drugs Co. Ltd. All right reserved.


Yang J.-L.,Hebei University of Science and Technology | Wang Q.-Y.,Hebei University of Science and Technology | Zhang Y.,Hebei University of Science and Technology | Zhang Y.,State Key Laboratory Breeding Base Key Laboratory of Molecular Chemistry for Drug of Hebei Province
Chinese Journal of New Drugs | Year: 2015

Objective: To improve the synthetic route of vildagliptin. Methods: L-proline was used as the starting material and treated by Boc-protection, amidation, dehydration, deprotection and N-chloroacetylation to give (S)-1-chloroacetyl-2-cyanopyrrolidine(2), which was then reacted with 3-amino-1-adamantanol to get the target product vildagliptin. Results: The structure of the target compound was confirmed by MS, 1H-NMR and 13C-NMR. The total yield was 32%, and the product purity was more than 99.8% as shown by HPLC analysis. Conclusion: The improved synthetic process with simplified operation, good yield and high purity is applicable for industrial production. ©, 2015, Chinese Journal of New Drugs Co. Ltd. All right reserved.

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