675126-27-9

基本信息
吉非替尼雜質(zhì)53
吉非替尼中間體N-1
2-氨基-4-甲氧基-5-(3-嗎啉丙氧基)苯腈
2-氨基-4-甲氧基-5-(3-嗎啉代丙氧基)芐腈
Gefitinib InterMediate
3-Methoxy-4-(3-(piperidin-1-yl)propoxy)benzonitrile
2-amino-4-methoxy-5-(3-morpholin-4-ylpropoxy)benzonitrile
2-amino-4-methoxy-5-[3-(4-morpholinyl)propoxy]benzonitrile
5-Methoxy-2-nitro-4-(3-(piperidin-1-yl)propoxy)benzonitrile
Benzonitrile,2-aMino-4-Methoxy-5-[3-(4-Morpholinyl)propoxy]-
物理化學(xué)性質(zhì)
制備方法

675126-26-8

675126-27-9
以4-甲氧基-5-(3-嗎啉丙氧基)-2-硝基苯甲腈為原料合成2-氨基-4-甲氧基-5-(3-嗎啉丙氧基)苯甲腈的一般步驟:將二亞硫酸鈉(89%,81.4 kg)加入攪拌中的4-甲氧基-5-(3-嗎啉丙氧基)-2-硝基苯甲腈(48.8 kg)的水(867 L)漿液中,將所得混合物加熱至50℃。反應(yīng)約2小時(shí)后完成。將反應(yīng)混合物的溫度升至約70℃,并在3小時(shí)內(nèi)緩慢加入濃鹽酸水溶液(36%,270 kg)。將所得混合物冷卻至20-25℃,同時(shí)繼續(xù)攪拌,并加入氫氧化鈉溶液(47%,303.7 kg)。用二氯甲烷(兩次,分別為1082 kg和541 kg)萃取反應(yīng)混合物,合并有機(jī)萃取物并用去離子水(510 L)洗滌。蒸發(fā)有機(jī)相,得到2-氨基-4-甲氧基-5-(3-嗎啉丙氧基)苯甲腈(46.3 kg,收率99%);熔點(diǎn)為87.5℃;核磁共振氫譜(DMSO-d6)δ:1.79(m,2H),2.36(t,4H),2.36(t,2H),3.56(t,4H),3.73(s,3H),3.86(t,2H),5.66(br s,2H),6.4(s,1H),6.89(s,1H);質(zhì)譜:M+H+ 292。
參考文獻(xiàn):
[1] Patent: WO2005/23783, 2005, A1. Location in patent: Page/Page column 18
[2] Patent: WO2004/24703, 2004, A1. Location in patent: Page 10
[3] Organic Process Research and Development, 2007, vol. 11, # 5, p. 813 - 816
[4] Patent: CN105503749, 2016, A. Location in patent: Paragraph 0053; 0054; 0055
[5] Patent: CN107586279, 2018, A. Location in patent: Paragraph 0008; 0018
報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
2025/05/22 | XW0267512627905 | 2-氨基-4-甲氧基-5-(3-嗎啉代丙氧基)芐腈 | 675126-27-9 | 25G | 1251元 |
2025/05/22 | XW0267512627904 | 2-氨基-4-甲氧基-5-(3-嗎啉代丙氧基)芐腈 | 675126-27-9 | 10G | 501元 |
2025/05/22 | XW0267512627903 | 2-氨基-4-甲氧基-5-(3-嗎啉代丙氧基)芐腈 | 675126-27-9 | 5G | 251元 |