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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
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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 .

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