A Simplified Process for the Manufacture of AZD0530, a Potent SRC Kinase Inhibitor

Steven A. Raw; Brian A Taylor; Simone Tomasi

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A Simplified Process for the Manufacture of AZD0530, a Potent SRC Kinase Inhibitor

机译：强大的SRC激酶抑制剂AZD0530的简化生产工艺

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An efficient process for the manufacture of AZD0530 1, a potent SRC kinase inhibitor, has been developed. The key transformation, reaction of monofluoroanilide 7 with alcohol 8, was much simplified between manufacturing campaigns. The development of a robust, efficient, and scalable process for this transformation drew on both a practical and theoretical understanding of the process and is described herein

机译：已经开发出有效的生产强效SRC激酶抑制剂AZD0530 1的方法。在制造活动之间，主要的转变是单氟苯胺7与醇8的反应大大简化了。针对该转换的健壮，有效和可扩展的过程的开发基于对过程的实践和理论理解，并在此进行描述

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《Organic process research & development》 |2011年第3期|共5页
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Steven A. Raw; Brian A Taylor; Simone Tomasi;
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1. A Simplified Process for the Manufacture of AZD0530, a Potent SRC Kinase Inhibitor [J] . Steven A. Raw, Brian A Taylor, Simone Tomasi Organic process research & development . 2011,第3期

机译：强大的SRC激酶抑制剂AZD0530的简化生产工艺
2. 361 Preclinical activity of AZD0530, a novel, oral, potent and selective inhibitor of the Src family kinases [J] . T.P.Green, M.Fennell, R.Whittaker, European Journal of Cancer Supplements . 2004,第8期

机译：361 AZD0530的临床前活性，AZD0530是新型，口服，有效和选择性的Src家族激酶抑制剂
3. Development of an Efficient and Practical Route for the Multikilogram Manufacture of the SRC Kinase Inhibitor AZD0530 [J] . J. Gair Ford, Anne OKearney-McMullan, Simon M. Pointon Organic process research & development . 2010,第5期

机译：开发有效且实用的路线来生产多公斤级SRC激酶抑制剂AZD0530
4. Taking Quinazoline as a General Support-Nog to Design Potent and Selective Kinase Inhibitors: Application to FMS-like Tyrosine Kinase 3 [C] . Wei-Wei Li, Luo-Ding Yu, Li-Juan Chen, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：以喹唑啉作为一般支持物来设计有效和选择性激酶抑制剂：在类似FMS的酪氨酸激酶3中的应用
5. Analysis of pp60c-src and pp62c-yes intracellular protein tyrosine kinase function in colon tumor cell growth regulation using herbimycin A, a tyrosine kinase specific inhibitor. [D] . Garcia, Roy. 1995

机译：使用酪氨酸激酶特异性抑制剂除草霉素A分析pp60c-src和pp62c-yes细胞内蛋白酪氨酸激酶在结肠肿瘤细胞生长调节中的功能。
6. Preclinical anticancer activity of the potent oral Src inhibitor AZD0530 [O] . Tim P. Green, Mike Fennell, Robin Whittaker, 2009

机译：有效的口服Src抑制剂AZD0530的临床前抗癌活性
7. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530 [O] . Green, Tim P., Fennell, Mike, Whittaker, Robin, 2009

机译：有效的口服src抑制剂aZD0530的临床前抗癌活性

A Simplified Process for the Manufacture of AZD0530, a Potent SRC Kinase Inhibitor

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