CAS: 5271-27-2; 1-Methyl-3-Phenylpiperazine

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CAS号23174-98-3 1-benzyl-4-meth... | CAS号799796-66-0 1-methyl-3-phen... | CAS号61338-13-4 米氮平酸 | CAS号61337-88-0 1-(3-氰基吡啶-2)-2-... | CAS号61337-89-1 2-(4-甲基-2-苯基-1-... | CAS号85650-52-8 米氮平 | CAS号333738-24-2 2-(4-methyl-3-p... | CAS号5271-29-4 1,4-dimethyl-2-...

1-苄基-4-甲基-2-苯基哌嗪置于5%-Palladium/activated Carbon 氢气,Sodium Hydroxide体系中,用 溶剂黄146,水 作为反应溶剂,25.0~30.0 °C,689.49 Kpa 条件下,反应 4.0H,反应生成 1-甲基-3-苯基哌嗪
参考文献:Process For Preparing 1-Methyl-3-Phenylpiperazine Using A Novel Intermediate
标题:Process For Preparing 1-Methyl-3-Phenylpiperazine Using A Novel Intermediate
摘要:本发明描述了一种工业上有利的工艺,用于制备高纯度的公式i1的1-甲基-3-苯基哌嗪,该工艺利用了一种新型哌嗪衍生物,4-苄基-1-甲基-2-氧代-3-苯基哌嗪,其化学式为ii2.1-甲基-3-苯基哌嗪是抗抑郁药米氮平的制备中有用的中间体.

专利信息

专利号:US-6852855-B2
优先权日:1999-04-19
标 题 :Synthesis of piperazine ring
发明人：DOLITZKY BEN-ZION
权利人:TEVA PHARMA
摘要:A novel process for preparing a compound of the formula I: n n nwhereinn nR 1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R 2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R 3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.

专利号:US-6603003-B2
优先权日:2000-11-07
标 题 :Method for the preparation of piperazine and its derivatives
发明人：SEBASTIAN SONNY; PATEL HETAL VIRENDRA; THENNATI RAJAMANNAR
权利人:SUN PHARMACEUTICAL IND LTD
摘要:A novel method for the synthesis of piperazine and its derivatives of formula 1,wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms;R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; andR2 is selected from hydrogen, or a methyl group, or a fluoromethyl group;comprising the steps:a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; andb. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.

专利号:EP-2038260-B1
优先权日:2006-06-16
标题:Stereoselective synthesis of (s)-1-methyl-3-phenylpiperazine
发明人：VAN VLIET MICHIEL CHRISTIAN ALEXANDER; KEMPERMAN GERARDUS JOHANNES; SCHREUDER GOEDHEIJT MARCEL
权利人:ORGANON NV
摘要:This invention provides for a compound according to Formula (1), wherein R1 is methyl, ethyl, n-propyl, isopropyl, benzyl or 2-haloethyl and the use thereof in a method to prepare (S)-1-methyl-3-phenylpiperazine by enzymatic hydrolysis of the compound, followed by separation and cleavage of the oxalamic groups, whereby the protease of Streptomyces griseus is used as enzyme for the enzymatic hydrolysis.

专利号:US-2002035256-A1
优先权日:1999-04-19
标题:Novel synthesis of piperazine ring

专利号:WO-0062782-A1
优先权日:1999-04-19
标题 :Novel synthesis and crystallization of piperazine ring-containing compounds
发明人：SINGER CLAUDE; LIBERMAN ANITA; FINKELSTEIN NINA
权利人:TEVA PHARMA; TEVA PHARMA; SINGER CLAUDE; LIBERMAN ANITA; FINKELSTEIN NINA
摘要:The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridly-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130 °C. The method of the present invention also includes reacting 2-amino-3-hydroxymethyl pyridine with N-methyl-1-phenyl-2, 2'-iminodiethyl chloride to form 1-(3-hydroxymethylpyridyl-2)-4-methyl-2-phenyl piperazine, and adding sulfuric acid to the 1-(3-hydroxymethylpyridyl-2)-phenyl-4-methylpiperazine to form mirtazapine. The present invention also relates to new processes for recrystallization of mirtazapine form crude mirtazapine.

专利号:US-6339156-B1
优先权日:1999-04-19
标题:Synthesis of piperazine ring