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2-[3-hydroxy-1-adamantyl]-2-oxoacetic acid [IV], a key intermediate of saxagliptin for type 2 diabetes mellitus [T2DM], was prepared from 1-adamantanecarboxylic acid[I] via oxidation by potassium permanganate[KMnO4] to afford 3-hydroxy-1-adamantanecarboxylic acid [II], which was treated with a one-pot method to give 1-acetyl-3-hydroxyadamantane [III] followed by oxidation. Some key steps were optimized and the overall yield was about 51%
RÉSUMÉ
OBJECTIVE:To construct integrated medication decision-making system,and to provide reference for safe,effec-tive,economical and reasonable drug use in clinic. METHODS:The construction of integrated medication decision-making system was introduced in our hospital. RESULTS&CONCLUSIONS:The integrated medication decision-making system included three as-pects as real-time intervention in advance,interactive review in the matter,afterward comment and analysis,as 3 steps before and after the implementation of inpatient medical order and outpatient prescription. The real-time intervention in advance was mainly to control the rationality of medical orders or prescriptions from their source,thus requiring the timely treatment. The interactive re-view in the matter required that pharmacists judged the medical order or prescription and made a decision of refusing prescribing within the fixed time. To make a decision accurately,the clinical information should be highly structured and correlated with drug signs. Afterward comment and analysis required that pharmacists evaluated the medical order or prescription regularly after the im-plementation. The three were not only different,but also coordinated,and they were an organic unity,especially interactive review in the matter needed to be coordinated with the other two processes. After the implementation of integrated medication decision-mak-ing system,the proportion of irrational medical orders or prescriptions in our hospital decreased from 6.07％ in the first half of 2016 to 2.56％ at corresponding period of 2017. Drug dose errors and incompatibility were greatly reduced,and medication against contraindications was more likely to be found in the review and analysis. The system can improve the efficiency of prescription re-view,improve rational drug use,and effectively ensure the safety,effectiveness,economy and rationality of clinical drug use.
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Pimavanserin(Nuplazid) is a drug of selective targeting 5-HT2A receptor,developed by Acadia Pharmaceuticals. In April 29,2016,it was approved by FDA for the treatment of Parkinson′s disease(PD)patients experiencing mental symptoms such as hallucinations and delusions. In this paper,we summarize the synthetic methods of pimavanserin published in literature in re?cent years and their advantages and disadvantages.
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Orphan nuclear receptor NR4A1 from the NR4A subfamily is one of the transcriptional factors that have not identified specific ligands .Previous studies have found that NR4A1 could regulate cell proliferation ,apoptosis ,differentiation and stress responses by changing gene expression ,post-translational modification and interactions between coregulatory pro-teins .Recently ,it has shown that NR4A1 has an abnormal expression in human atherosclerotic lesions and has been identified as a key regulator gene in vascular cells dysfunction .Regulating NR4A1 expression can have an important impact on the prolif-eration of smooth muscle cell and endothelial cell activation ,meanwhile it could reduce inflammation ,foam cell formation and lipid deposition ,inhibit vascular remodeling ,and prevent the development of atherosclerosis .These studies suggest that NR4A1 might be a novel target for drug development in prevention and treatment of atherosclerosis .
RÉSUMÉ
Pimavanserin(Nuplazid) is a drug of selective targeting 5-HT2A receptor, developed by Acadia Pharmaceuticals. In April 29, 2016, it was approved by FDA for the treatment of Parkinson’s disease (PD) patients experiencing mental symptoms such as hallucinations and delusions. In this paper, we summarize the synthetic methods of pimavanserin published in literature in recent years and their advantages and disadvantages.
RÉSUMÉ
Objective To synthesize the impurity of vildagliptin as a reference substance, and optimize its preparation process by the central composite design-response surface methodology. Method The impurity was synthesized from L-proline and 3-amino-1-adamantanol through chloroacetylation, amination, dehydration and substitution. Results The structure of the disubstituted derivative of vildagliptin was verified by IR, 1H-NMR and MS. Conclusion The synthesized compound can be used as the reference substance of the impurity, so the impurity can be controlled. Preparation process gained the application value after it was optimized by the central composite design-response surface methodology.