1022150-11-3
1022150-11-3 結(jié)構(gòu)式
基本信息
依魯替尼雜質(zhì)47
依魯替尼雜質(zhì)BOC
依魯替尼雜質(zhì)1對照品
[3,4-D]嘧啶-1-基]哌啶-1-羧酸叔丁酯
(R)-3-[4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶-1-基]哌啶-1-羧
(R)-1-(1-BOC-3-哌啶基)-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶-4-胺
(R)-3-[4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶-1-基]哌啶-1-羧酸叔丁酯
(R)-3-[4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-D]嘧啶-1-基]哌啶-1-羧酸叔丁酯 IBL6
N-BOC-IBRUTINIB ( TERT-BUTYL-1-CARBOXYL PIPERIDINE ANALOG OF IBRUTINIB)
Ibrutinib iMpurity Boc
Ibrutinib Intermediates
(R)-tert-butyl 3-(4-amino-3-(4-phenoxyphenyl)-
3-[4-Amino-3-(4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-y...
N-Boc-Ibrutinib ( tert-Butyl-1-carboxyl Piperidine analog of Ibrutinib)
(R)-1-(1-Boc-3-piperidinyl)-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
(R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-ca
(R)-3-[4-Amino-3-(4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]-piperidine-1-carboxylic acid
tert-butyl (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate
物理化學(xué)性質(zhì)
制備方法
![(3R)-1-BOC-3-(4-氨基-3-碘-1H-吡唑并[3,4-D]嘧啶-1-基)哌啶](/CAS/20150408/GIF/1276110-38-3.gif)
1276110-38-3
51067-38-0
1022150-11-3
步驟4A: 在氮氣保護下，將(R)-3-(4-氨基-3-碘-1H-吡唑并[3,4-d]嘧啶-1-基)哌啶-1-甲酸叔丁酯（1g，2.25mmol，1.00當(dāng)量）、4-苯氧基苯基硼酸（530mg，2.48mmol，1.10當(dāng)量）、碳酸鈉（480mg，4.53mmol，2.01當(dāng)量）和四（三苯基膦）鈀（78mg，0.07mmol，0.03當(dāng)量）溶于二惡烷（60mL）和水（15mL）的混合溶劑中。將反應(yīng)混合物在90℃下攪拌24小時。反應(yīng)完成后，將混合物冷卻至室溫，隨后在減壓下濃縮。將殘余物溶解于二氯甲烷（500mL）中，所得溶液用水（200mL）洗滌，無水硫酸鈉干燥，再次減壓濃縮。粗產(chǎn)物通過硅膠柱色譜法純化，洗脫劑為二氯甲烷/甲醇（100/1，v/v），得到700mg（產(chǎn)率64%）的(R)-3-(4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶-1-基)哌啶-1-甲酸叔丁酯，為黃色固體。
參考文獻(xiàn)：
[1] Patent: WO2012/158795, 2012, A1. Location in patent: Page/Page column 76
[2] Patent: WO2013/191965, 2013, A1. Location in patent: Page/Page column 156
[3] Patent: WO2014/22569, 2014, A1. Location in patent: Page/Page column 50
[4] Patent: US8673925, 2014, B1. Location in patent: Page/Page column 201
[5] Patent: CN106146511, 2016, A. Location in patent: Paragraph 0150; 0151; 0152