Dissertation > Excellent graduate degree dissertation topics show

The Research on Synthesis of Mirtazapine and Its Intermediates

Author: XiuWenHua
Tutor: LinYuanBin
School: Xiangtan University
Course: Organic Chemistry
Keywords: Mirtazapine 1 - methyl -3 - phenylpiperazine Cyclization reaction
CLC: TQ463
Type: Master's thesis
Year: 2004
Downloads: 395
Quote: 0
Read: Download Dissertation

Abstract


Mirtazapine Mirtazapine ( aka Remeron remernon ) Chemical name : 1,2,3,4,10,14 b- hexahydro -2 - methyl- pyrazinyl [ 2,1- a ] pyrido [2,3 -c] benzodiazepine , is the development of a new generation of antidepressants by Organon , the Netherlands , in the clinical treatment effect . Styrene oxide , N-methyl ethylenediamine pyridine and 2 - chloro-3 - nitrile group as the basic raw material , through intensive research on the reaction conditions , the synthesis of the target product mirtazapine , closing after eight -step reaction rate of 3% , purity 99% (GC) ( the literature total yield 13.3%) ; Patent Document 1 - methyl-3 - phenyl - piperazine and its intermediates in synthetic methods were improved in the ring closure step , using the indirect method (i.e., low temperature amination , high temperature cyclization methods) , improved product purity ( ≥ 99 % ) and yield ( 19.4%) ; styrene oxide is enhanced through the introduction of a large volume of a group on the nucleophilic reagent , the selectivity of the β-position , to solve the difficult problem of separating isomers exist in the literature , synthetic intermediates of high purity ( 99%) of 1 - methyl - 3 - phenyl- piperazine , yield better ( 30% ), provide a good reference for the series of substituted piperazine ; synthesis of a series of alpha , beta -substituted pyridine derivatives, with petroleum ether and purified by recrystallization of the intermediate 2 - chloro-3 - carbonitrile pyridine avoid the literature using high vacuum purification methods , easy to operate , high purity of the resulting product (99%) ; via the synthesis of 2 - chloro - nicotinic acid and 1 - methyl - 3 - phenyl piperazine one step intermediate 1 - ( 3 - carboxylic acid - 2 - pyridyl ) -4 - methyl-2 - phenyl - piperazine . The mild reaction conditions , to avoid literature use large amounts of acids, alkalis , and shorten the reaction time . Inadequacies lower yield ( about 30%) , the reaction conditions to be improved; first 1 - (3 - carboxylic acid -2 - pyridyl ) -4 - methyl-2 - phenyl- piperazine as the raw materials used FC reaction - Huangminglong reduction method Synthesis endproducts mirtazapine . This method avoids the use of expensive reducing reagent the LiAlH4, more suitable for industrial production .

Related Dissertations

  1. Synthesis and antidepressant drug intermediates PVDF fluorocarbon resin coating method for the determination of,TQ630.7
  2. Stress stimulation early drug interventions to prevent post-traumatic stress disorder in rats experimental study,R749.5
  3. Studies on the Asymmetric Synthesis of Cryptopyranmoscatone A1-A3 and Goniothalesdiol A,O621.3
  4. Synthetic Effects of Antidepressants on a Pancreatic Cancer Mouse Model and Adjunctive Effects of Antidepressants on Chemotherapy and Photodynamic Therapy,R735.9
  5. Novel Strategy for Synthesis of 5,7-dichloroindole Derivatives,TQ25
  6. Study on Synthetic Technology of the New Antidepressant Drug-Mirtazapine,TQ463
  7. The Application of Sulfinatodehalogenation in Synthesis and Transformation of Fluoroalkylated Porphyrins,O621.25
  8. Studies on the Transition Metal Catalyzed Cyclization and Addition Reaction of Acetylenes,O643.32
  9. Studies on the Synthesis of Natural Bis-indole Alkaloid Analogs and on the Cyclization of α, β-unsaturated Indolones,R914
  10. Study on the Changes of Monamine Transmitters and Their Receptors in Post-stroke Depression Rats and Protective Mechanisms of Mirtazapine,R749.1
  11. Studies on Palladium-Catalyzed Cyclization Reactions,O643.32
  12. Synthesis of Osmabenzenes and Ruthenabenzenes Based on [5+1] Cyclization Reaction,O621.2
  13. Study on Domino Reaction of 2-(2-Alkynylarylidene)-1,3-Dicarbonyl Compounds,O621.2
  14. Transition Metal-induced Activation of Alkynes Leading to Cyclization Reactions,O621.256.9
  15. Thiocyanation of Aromatic and Heteroaromatic Compounds and Aromatization of Pyrazolines,O621.25
  16. Study on the Synthesis of Nitric Heterocyclic Ring Compound and Its Derivatives,O626
  17. Study on the Preparation and Cyclization Reaction of 5-o-tolyl-2-pentene,TQ241.2
  18. Quantitative Analyses of Valsartan and Mirtazapine in Plasma and Their Applications in Pharmacokinetic Studies,R96
  19. PAN pre-oxidized fiber carbonization tar elimination and control,TQ343.6
  20. Application Research of 2-Hydroxyalkyl Phenyl Selenide Reagents in Organic Synthesis,O621.3

CLC: > Industrial Technology > Chemical Industry > Pharmaceutical chemical industry > Production of organic compounds in drug
© 2012 www.DissertationTopic.Net  Mobile