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首页> 外文期刊>Organic process research & development >A Review of U.S. Patents in the Field of Organic Process Development Published During April and May 2007
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A Review of U.S. Patents in the Field of Organic Process Development Published During April and May 2007

机译：2007年4月至5月发表的有机工艺开发领域的美国专利综述

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This latest review of U.S. patents contains 21 from an initial set of 264 that fitted the search criteria. Previously the majority of the patents chosen have been selected by the editor, but as an experiment all of the current patents were selected by the reviewer. Hence even though readers may notice a difference in the focus of the subjects of the patents that have been chosen, it is hoped there are still some of interest. A new process is reported for the insecticide gemifloxacin using an intensive mixing method that has the capability of dramatically improving productivity. Another patent on insecticides describes some novel malonic ester intermediates that are used to prepare indanecarboxylates, intermediates used; to prepare insecticides. Treatments for coronary diseases feature; one patent reports a range of novel diphenylazetidinones for treating high levels of cholesterol, while another reports on a new process for preparing the angina drug amlodipine. A third reports on two new processes for making perindopril, an inhibitor of angiotensin-converting enzymes used in cardiovascular treatments. Novel indazole compounds are reported for treating neurological diseases and the production of cabergoline for the treatment of Parkinsonism is reported, while another describes a range of isoquinolinyl indoles for treating dementia. Diabetes is the subject of two patents, with one providing very extensive details for preparing some novel phenoxazines. The other patent reports on benzotriazoles that are useful in treating non-insulin-dependent diabetes. Cancer treatments are understandably widely studied, and a range of tetrahydropyrimidines has been found to assist apoptosis by crossing cell membranes in a manner similar to ceramides. Another patent describes over 150 compounds that are intermediates or potential topisomerase-targeting agents and hence of use in cancer treatments. Novel pyrrolidines have been found that are said to be useful for treating asthma without the side effects associated with other drugs. An improvement in the bioavailability of the COX-2 inhibitor celecoxib by the manufacturers is described. This is made possible by producing an amorphous form of the drug in a simple procedure, but whether it is in use is not known. A novel method of producing tadalafil, for treating erectile dysfunction, is described. The new method reduces significantly the processing time and avoids the use of corrosive reagents. Moving away from pharmaceuticals, there is a process for producing fluorinated diols used in making advanced photoresist materials. Light-emitting diodes are important in many electronic devices, and a new process of preparing benzothiadiazoles is described that uses reagents less hazardous than alternative methods. The Kumada coupling reaction is a very widely used reaction, and it has been applied to an improved synthesis of 3-alkylthiophenes by simply changing the solvent. Also on the subject of 3-substituted thiophenes is a patent that describes how 3-halothiophenes can be produced by isomerisation of thereadily available and cheaper 2-isomer. There is no legal or commercial significance in the choice of patents, although some do describe experiments on moderate to large scale. This may suggest advanced development or commercial activity. In fact the newly described process for gemifloxacin is suggested as being capable of being used to produce 1500 kg per week of the product. The advantages described in this review are those claimed in the patent unless this reviewer has personal knowledge of the subject.
机译：美国专利的最新审查包含符合搜索标准的最初264套中的21套。以前，所选的大多数专利都是由编辑选择的，但是作为实验，所有当前的专利都是由审阅者选择的。因此，即使读者可能会注意到所选专利主题的重点有所不同，也希望仍然有一些兴趣。报道了一种使用强力混合法的杀虫剂吉非沙星的新工艺，该工艺具有显着提高生产率的能力。关于杀虫剂的另一项专利描述了一些新的丙二酸酯中间体，这些中间体用于制备茚满羧酸酯，所用中间体;准备杀虫剂。冠状动脉疾病的治疗方法;一项专利报告了一系列用于治疗高水平胆固醇的新型二苯基氮杂环丁酮，而另一项专利则报告了一种制备心绞痛药物氨氯地平的新工艺。第三份报告报道了两种新的制备培哚普利的方法，培哚普利是一种用于心血管疾病的血管紧张素转换酶抑制剂。据报道新型吲唑化合物可用于治疗神经系统疾病，卡麦角林的生产可用于治疗帕金森氏症，而另一种化合物则描述了一系列异喹啉基吲哚类药物用于治疗痴呆症。糖尿病是两项专利的主题，其中一项专利提供了制备某些新型吩恶嗪的非常详尽的细节。其他专利报告了可用于治疗非胰岛素依赖型糖尿病的苯并三唑。可以理解，对癌症的治疗方法已经进行了广泛的研究，并且发现了一系列四氢嘧啶可以通过类似于神经酰胺的方式穿过细胞膜来辅助细胞凋亡。另一项专利描述了超过150种化合物，它们是中间体或潜在的拓扑异构酶靶向剂，因此可用于癌症治疗。已发现新型吡咯烷类化合物可用于治疗哮喘，而没有其他药物带来的副作用。描述了制造商对COX-2抑制剂塞来昔布的生物利用度的改善。通过以简单的程序生产无定形形式的药物可以做到这一点，但尚不清楚它是否在使用中。描述了一种生产他达拉非的新方法，用于治疗勃起功能障碍。新方法大大减少了处理时间，并避免了使用腐蚀性试剂。远离药物，有一种生产用于制造高级光致抗蚀剂材料的氟化二醇的方法。发光二极管在许多电子设备中都很重要，并且描述了一种制备苯并噻二唑的新方法，该方法使用的危险性低于替代方法。熊田偶联反应是非常广泛使用的反应，并且已经通过简单地改变溶剂将其应用于改进的3-烷基噻吩的合成。关于3-取代的噻吩的主题也是专利，该专利描述了如何通过将可用的和便宜的2-异构体异构化来生产3-卤代噻吩。专利的选择没有法律或商业意义，尽管有些确实描述了中到大规模的实验。这可能暗示了先进的开发或商业活动。实际上，新描述的吉非沙星工艺被建议能够每周生产1500公斤产品。除非该审阅者对主题有个人知识，否则本审阅中所述的优点是专利所要求的优点。

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