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1. 发明授权

US07960545B2 Process for the prepartion of erlotinib 有权
标题翻译：厄洛替尼的制备过程
公开(公告)号：US07960545B2
公开(公告)日：2011-06-14
申请号：US12094926
申请日：2006-11-22
申请人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D239/72
CPC分类号： C07D239/94
摘要： The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1a) with a HPLC purity of >99.8%. Erlotinib hydrochloride is useful for the treatment of proliferative disorders, such as cancers, in humans.
摘要翻译：本发明公开了一种制备式（1）的厄洛替尼（N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺）的改进和新颖的方法，其包括：（i）市售的式（8）的6,7-二甲氧基-4（3H） - 喹唑啉酮的脱甲基化; 使用乙酸酐乙酰化; （iii）在喹唑啉酮的C-4位引入离去基团; （iv）与3-乙炔基苯胺缩合得到新的式（12）化合物; （v）脱乙酰化得到式（13）的新型二羟基化合物; 和（vi）用2-碘乙基甲基醚O-烷基化得到式（1）的厄洛替尼碱。埃洛替尼碱通过乙酸乙酯重结晶纯化，得到HPLC纯度> 99.5％。用氯化氢盐形成该碱，得到HPLC纯度> 99.8％的药学上可接受的式（1a）盐酸阿洛替尼。盐酸埃罗替尼可用于治疗人类增殖性疾病，如癌症。

2. 发明申请

US20110039844A1 6-7,DIALKOXY QUINAZOLINE DERIVATIVES USEFUL FOR TREATMENT OF CANCER RELATED DISORDERS 有权
标题翻译： 6-7，适用于治疗癌症相关疾病的DIALKOXY喹唑啉衍生物
公开(公告)号：US20110039844A1
公开(公告)日：2011-02-17
申请号：US12812726
申请日：2008-01-18
申请人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Satya , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Satya , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/5377 , C07D413/12 , A61P35/00
CPC分类号： A61K31/5377 , C07D239/94
摘要： In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A).
摘要翻译：鉴于喹唑啉类化合物具有巨大的潜力，我们开始对大量具有新型结构特征的新化学物质进行合成和筛选。出人意料地发现，与喹唑啉类的其他显着成分相比，在第4位具有3-乙炔基苯胺基的6和7位上具有特异性取代的烷氧基的喹唑啉具有很强的增强和特殊的抗增殖特性的药物。此外，令人惊讶的是，本发明的化合物毒性远低于安全性，对于治疗应用是非常有益的。本发明中描述的新颖化学实体由通式结构（I）表示，并没有早期合成，也没有对其治疗益处和安全性进行调查。当结构（A）时，化合物（I）是NRC-2694。

3. 发明申请

US20090306377A1 NOVEL PROCESS FOR THE PREPARTION OF ERLOTINIB 有权
标题翻译：用于制备ERLOTINIB的新方法
公开(公告)号：US20090306377A1
公开(公告)日：2009-12-10
申请号：US12094926
申请日：2006-11-22
申请人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1a) with a HPLC purity of >99.8%. Erlotinib hydrochloride is useful for the treatment of proliferative disorders, such as cancers, in humans.
摘要翻译：本发明公开了一种制备式（1）的厄洛替尼（N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺）的改进和新颖的方法，其包括：（i）市售的式（8）的6,7-二甲氧基-4（3H） - 喹唑啉酮的脱甲基化; 使用乙酸酐乙酰化; （iii）在喹唑啉酮的C-4位引入离去基团; （iv）与3-乙炔基苯胺缩合得到新的式（12）化合物; （v）脱乙酰化得到式（13）的新二羟基化合物; 和（vi）用2-碘乙基甲基醚O-烷基化得到式（1）的厄洛替尼碱。埃洛替尼碱通过乙酸乙酯重结晶纯化，得到HPLC纯度> 99.5％。用氯化氢盐形成该碱，得到HPLC纯度> 99.8％的药学上可接受的式（1a）盐酸阿洛替尼。盐酸埃罗替尼可用于治疗人类增殖性疾病，如癌症。

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