化学研究与应用
化學研究與應用
화학연구여응용
CHEMICAL RESEARCH AND APPLICATION
2013年
8期
1180-1184
,共5页
孙键%李娇毅%张喜全%顾红梅%杨玲%李宝林
孫鍵%李嬌毅%張喜全%顧紅梅%楊玲%李寶林
손건%리교의%장희전%고홍매%양령%리보림
吉非替尼%异香兰素%4-甲氧基-3-(3-氯丙氧基)苯甲腈%2-硝基-4-甲氧基-5-(3-氯丙氧基)苯甲腈%2-氨基-4-甲氧基-5-(3-氯丙氧基)苯甲腈
吉非替尼%異香蘭素%4-甲氧基-3-(3-氯丙氧基)苯甲腈%2-硝基-4-甲氧基-5-(3-氯丙氧基)苯甲腈%2-氨基-4-甲氧基-5-(3-氯丙氧基)苯甲腈
길비체니%이향란소%4-갑양기-3-(3-록병양기)분갑정%2-초기-4-갑양기-5-(3-록병양기)분갑정%2-안기-4-갑양기-5-(3-록병양기)분갑정
Gefitinib%isovanillin%3-( 3-chloropropoxy )-4-methoxybenzonitrile%2-nitro-5-( 3-chloropropoxy )-4-methoxybenzonitrile%2-amino-5-(3-chloropropoxy)-4-methoxybenzonitrile
以异香兰素为原料，通过氰基化、氯烷基化、硝化、还原、Dimroth重排和吗啉基的引入六步反应，高收率地合成了抗肿瘤药物吉非替尼。所得各种中间体化合物及吉非替尼均经波谱学方法鉴定，六步反应总收率为49.8％。该合成方法高效、简捷，适用于工业化生产。
以異香蘭素為原料，通過氰基化、氯烷基化、硝化、還原、Dimroth重排和嗎啉基的引入六步反應，高收率地閤成瞭抗腫瘤藥物吉非替尼。所得各種中間體化閤物及吉非替尼均經波譜學方法鑒定，六步反應總收率為49.8％。該閤成方法高效、簡捷，適用于工業化生產。
이이향란소위원료，통과청기화、록완기화、초화、환원、Dimroth중배화마람기적인입륙보반응，고수솔지합성료항종류약물길비체니。소득각충중간체화합물급길비체니균경파보학방법감정，륙보반응총수솔위49.8％。해합성방법고효、간첩，괄용우공업화생산。
Gefitinib was synthesized from isovanillin as the starting material by six-step reactions including cyanidation ,chloroalkyla-tion,nitration,reduction,Dimroth rearrangement and amination with morpholine .The structures of synthesized intermediates and ge-fitinib were identified by spectroscopy .The total yield of six-steps was 49.8%.This method was suitable for industrial production with the advantages of efficient and simple .
