Dongguan, China
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Zhang J.,HEC Pharm Group | Nie B.,HEC Pharm Group | Zhang Y.,HEC Pharm Group
Chinese Journal of Organic Chemistry | Year: 2015

This article reviews the application and progress of modern synthetic methods to deliver several innovative drugs, especially the blockbusters, such as sofosbuvir, rivaroxaban, enzalutamide, canagliflozin and tofacitinib. Some of the modern synthetic methods, for example catalytic processes, application of ring-closing metathesis, palladium catalyzed cross-coupling, green chemistry and telescoping of processes, are highlighted. The exciting journey from discovering these new molecular entities, especially those which are first-in-class with the synthesis of a dozen of approved drugs, is described as case studies to fully illustrate the important role of modern organic synthesis for successful drug discovery and development. © 2015 Chinese Chemical Society & SIOC, CAS.

Zhang J.,HEC Pharm Group | Jin C.,HEC Pharm Group | Zhang Y.,HEC Pharm Group
Chinese Journal of Organic Chemistry | Year: 2014

This review outlines the recent advances of fluorinated drugs and latest research overview from the perspective of a medicinal chemist wherein the synthesis and use of trifluoromethylation, difluoromethylation, monofluoromethylation and fluorinated aromatic (heterocyclic) compounds are highlighted. It is pointed out that the full use of the latest progress in fluorine chemistry provides a shortcut to new fluorinated compounds or previously difficult to prepare compounds which is worth exploring for drug discovery. © 2014 Chinese Chemical Society & SIOC, CAS.

Yang X.,HEC Pharm Group | Xiong X.,HEC Pharm Group | Cao J.,HEC Pharm Group | Luan B.,HEC Pharm Group | And 3 more authors.
Journal of Chromatography A | Year: 2015

Matrix interference, which can lead to false positive/negative results, contamination of injector or separation column, incompatibility between sample solution and the selected analytical instrument, and response inhibition or even quenching, is commonly suffered for the analysis of trace level toxic impurities in drug substance. In this study, a simple matrix precipitation strategy is proposed to eliminate or minimize the above stated matrix interference problems. Generally, a sample of active pharmaceutical ingredients (APIs) is dissolved in an appropriate solvent to achieve the desired high concentration and then an anti-solvent is added to precipitate the matrix substance. As a result, the target analyte is extracted into the mixed solution with very less residual of APIs. This strategy has the characteristics of simple manipulation, high recovery and excellent anti-interference capability. It was found that the precipitation ratio (R, representing the ability to remove matrix substance) and the proportion of solvent (the one used to dissolve APIs) in final solution (P, affecting R and also affecting the method sensitivity) are two important factors of the precipitation process. The correlation between R and P was investigated by performing precipitation with various APIs in different solvent/anti-solvent systems. After a detailed mathematical reasoning process, P= 20% was proved to be an effective and robust condition to perform the precipitation strategy. The precipitation method with P= 20% can be used as a general strategy for toxic impurity analysis in APIs. Finally, several typical examples are described in this article, where the challenging matrix interference issues have been resolved successfully. © 2014 Elsevier B.V.

Zhang J.,HEC Pharm Group | Zhang Y.,HEC Pharm Group
Chinese Journal of Organic Chemistry | Year: 2013

The recent synthetic development and applications of mucochloric acid, mucobromic acid and their derivatives are described, mainly focus on our work using these multiple functional molecules to access a wide variety of γ-butenolides, γ-lactams, 4, 5-dihalopyridazin-3-ones and other novel, multi-functionalized building blocks and pharmaceutical products. © 2013 Chinese Chemical Society and SIOC, CAS.

Zhang Y.,HEC Pharm Group | Nie B.,HEC Pharm Group | Zhang J.,HEC Pharm Group
Chinese Journal of Organic Chemistry | Year: 2015

The copper-catalyzed C-H activation, selective functionalization and the development of cyclization strategy for the synthesis of novel fused-heterocyclic (heterocycles with ring-junction nitrogen or bridgehead nitrogen) compounds are discussed. This class of novel bridgehead nitrogen heterocycles includes indolizine, pyrazolopyridine, benzimidazole and other polyheterocyclic compounds. The series including modern amination, oxidative coupling and Csp2-H, Csp-H, Csp3-H and N-H activation catalyzed by Cu(I) or Cu(II) salts makes this green synthesis a superior and practical method providing entry into complex heterocycles. Some reaction mechanisms have also been summarized. © 2015 Chinese Chemical Society & SIOC, CAS.

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