CAS: 430461-56-6; (R)-3-Phenylpiperidine

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CAS号430461-53-3 2-tert-butyl-3-... | CAS号56613-80-0 D-苯甘氨醇 | CAS号343947-52-4 methyl 5-oxo-4-... | CAS号332-15-0 1-Styrylpiperidine | CAS号122-78-1 2-苯基乙醛 | CAS号430461-23-7 (3R,8R,8aR)-3,8... | CAS号4663-33-6 反式-1,3-二苯基-2-丙烯-1-醇

合成工艺路线路线简述

  • 合成目标产物 R)-3-Phenyl Piperidine 主要起始原料 3-Phenylpiperidine
  • (文献来源)合成步骤主要原料 3-Phenylpiperidine
📜Ethyl (E)-1,3-Diphenyl-2-Propen-1-Yl Carbonate置于rucl2(1,3-Dimesityl-Imidazolidin-2-yl)(Pcy3)(=chph),Palladium On Activated Charcoal,Bis(η3-Allyl-μ-Chloropalladium(II)) 苯磺酰胺,Samarium Diiodide,Aspartic Acid-Derived P-Chirogenic Diaminophosphine Oxide,氢气,N,N-二异丙基乙胺体系中,用 四氢呋喃,甲醇,乙醇,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 15.5H,反应生成 (R)-3-苯基哌啶
参考文献:钯催化的手性二氨基膦氧化物与硝基甲烷的不对称烯丙基烷基化反应:(s,R P)-Ph-Diaphox.(R)-Preclamol和(R)-Baclofen的对映选择性合成
标题:钯催化的手性二氨基膦氧化物与硝基甲烷的不对称烯丙基烷基化反应:(s,R P)-Ph-Diaphox.(R)-Preclamol和(R)-Baclofen的对映选择性合成
摘要:描述了使用天冬氨酸衍生的p-手性二氨基膦氧化物[(s,R P)-Ph-Diaphox]与硝基甲烷进行pd催化的不对称烯丙基烷基化反应.该方法已成功应用于对映异构体合成(R)-Preclamol和(R)-Baclofen.
DOI:10.1016/j.Tetlet.2006.07.029

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专利信息


专利号:WO-2019165981-A1
优先权日:2018-03-02
标 题:Methods for synthesizing (r)-3-phenylpiperidine or/and (s)-3-phenylpiperidine and chiral intermediates of niraparib
发明人:LIU ZHENDE; GAO HEYONG
权利人:SHANGHAI BIOBOND PHARMACEUTICAL CO LTD
摘要:The synthesis method provided by the first aspect of the invention successfully prepares the target product (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine using a N-protected 3-piperidone as a starting material. The synthesis method provided by the second aspect of the invention successfully prepares the target product (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine using the same starting raw material with the ingenious use of an organic silicon reagent. The (S)-3-phenylpiperidine can be used to synthesize the chiral intermediate α, β or γ of niraparib according to the third, the fourth or the fifth aspect of the invention, respectively. In general, the methods for synthesizing (R)-3-phenylpiperidine or/and (S)-3-phenylpiperidine and the chiral intermediates α, β and γ of niraparib significantly reduces the production cost, favoring the large-scale industrial production of niraparib.

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