29608-05-7

基本信息
4-(1-哌啶基甲基)苯胺
4-(PIPERIDIN-1-YLMETHYL)ANILINE
4-PIPERIDIN-1-YLMETHYL-PHENYLAMINE
AKOS B014375
AKOS MSC-0180
ART-CHEM-BB B014375
ART-CHEM-BB B016020
ASISCHEM W54645
TIMTEC-BB SBB007056
4-(Piperidin-1-ylmethyl)aniline 95%
4-(Piperidylmethyl)phenylamine
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法

59507-44-7

29608-05-7
以1-(4-硝基芐基)哌啶為原料合成4-哌啶-1-甲基苯胺的一般步驟:向4-硝基芐基氯(1 mmol)的無(wú)水THF(3 mL)溶液中依次加入1-甲基哌嗪或哌啶(1 mmol)和三乙胺(1.5 mmol,0.21 mL)。將反應(yīng)混合物于70℃下攪拌反應(yīng)過(guò)夜。反應(yīng)完成后,用二氯甲烷和水進(jìn)行萃取。合并有機(jī)相,用無(wú)水Na2SO4干燥,減壓濃縮除去溶劑。通過(guò)柱色譜法(洗脫劑:己烷/乙酸乙酯,1:4)純化殘余物,并通過(guò)1H NMR(參見(jiàn)補(bǔ)充信息)進(jìn)行結(jié)構(gòu)表征。將純化后的產(chǎn)物溶解于乙醇(10 mL)中,在氮?dú)獗Wo(hù)下加入PtO2(0.01 g)。在Parr氫化裝置中,于50 psi氫氣壓力下氫化16小時(shí)。反應(yīng)結(jié)束后,過(guò)濾除去催化劑,濾液經(jīng)真空濃縮,得到目標(biāo)產(chǎn)物4-哌啶-1-甲基苯胺,收率定量。
參考文獻(xiàn):
[1] European Journal of Medicinal Chemistry, 2011, vol. 46, # 7, p. 2917 - 2929
[2] RSC Advances, 2015, vol. 5, # 58, p. 47125 - 47130
[3] Journal of Medicinal Chemistry, 2016, vol. 59, # 20, p. 9409 - 9421
[4] Patent: CN106432235, 2017, A. Location in patent: Paragraph 0113
[5] Patent: WO2006/12135, 2006, A1. Location in patent: Page/Page column 54-56