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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 December 2010 and January 2011
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A Review of U.S. Patents in the Field of Organic Process Development Published During December 2010 and January 2011

机译：2010年12月至2011年1月发表的有机工艺开发领域的美国专利综述

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摘要

The current selection of patents contains 20 from an original list containing 267 that fitted the selection criteria. Some patents have a considerable amount of experimental detail and space limits the amount that can be included in the review. On the other hand, there are others that have so little detail that it is difficult to accept the claims in the patent. An example is a new process for the preparation of pramipexole, a drug used to treat Parkinson's disease and schizophrenia. The patent claims two novel compounds that are intermediates but provides no physical properties or spectral details for them whatsoever. Another example of lack of detail is in a patent describing a process to prepare pyran compounds that can be used in flavours and perfumes. None of the examples give details of the scale of the experiment nor provide information on the quantities of reagents used; however, there is plenty of spectral data. An example of an abundance of details is a very comprehensive patent on statins that describes several novel intermediates and gives detailed experimental information and spectral details for them all. Two patents from different companies cover novel polymorphs of the antiparasitic agent atovaquone, and it seems that the new polymorphs are all different. A method of improving a process by reducing the number of stages is usually cost-effective but can result in handling problems. For example, a one-step method of making phenothiazine alkylsulfonate derivatives uses very potent carcinogenic sultone compounds. A process that does eliminate the use of hazardous and toxic reagents is exemplified by a patent describing a method to purify ropinirole, another drug used to treat Parkinsonism. The patent describes a means of removing coloured impurities, but it is not clear which reagent is actually used and hence what is the basis of the invention. A process for preparing a high-purity fluoroisoquinoline salt is described that avoids the use of diazonium salts that can be unstable. The removal or minimisation of organic solvents is an area of great activity, and a process for preparing imidazole-2-thiones does not use solvents and generally starts from liquid reagents. In cases where this is not possible or the product is a solid, then a melting point depressant is added to the reaction mixture, and the product yields are very good. A process for producing an enriched mixture of the aroma chemical isopulegol uses the technique of melt crystallisation that also avoids the use of solvents. The purification of an intermediate used to prepare a thiazole pesticide is generally by distillation, but azeotropes can be formedby some reaction impurities. By removing these before distillation the process is improved. Ionic liquids are of interest as reagents and solvents, and a new process claims to produce such compounds with virtually any anion and with very low levels of impurities. Oxycodone is used to relieve severe pain after surgery, and two patents describe methods for removing Michael acceptor impurity levels in the drug. There does appear to be some overlap in the two processes that may result in a legal dispute between the parties. Halogenation reactions can give rise to waste disposal or safety problems, and two patents address such concerns. One replaces 1,2-diiodoethane in an iodination step with F5C5I in the synthesis of pyrazole antidepressants, and the other improves the production of dibromodiamantane by using AlBr3 and Br2. In two separate patents new methods are described for the preparation of the antipsychotic drugs quetiapine and asenapine. A range of sugar derivatives of benzimidazole compounds is described that are antivirals, and a new route for preparing the antiemetic drug dolasteron is disclosed that involves novel intermediates. A number of the patents in this collection describe experiments carried out on a kilo or multikilo scale, and this may suggest an. advanced stage of development or even comm
机译：当前选择的专利中，有267个符合选择标准，而原始列表中有20个。一些专利具有大量的实验细节，并且篇幅限制了可以包括在本评论中的数量。另一方面，还有一些细节很少，以致难以接受专利中的权利要求。一个例子是制备普拉克索的新工艺，普拉克索是一种用于治疗帕金森氏症和精神分裂症的药物。该专利要求保护两种新颖的化合物，它们是中间体，但是无论如何都没有提供物理性质或光谱细节。缺乏细节的另一个例子是在专利中描述了一种制备可用于调味剂和香料中的吡喃化合物的方法。这些实施例均未提供实验规模的细节，也未提供所用试剂的量的信息。但是，有很多光谱数据。大量细节的一个例子是关于他汀类药物的非常全面的专利，该专利描述了几种新型中间体，并为它们提供了详细的实验信息和光谱详细信息。来自不同公司的两项专利涵盖了抗寄生虫药atovaquone的新型多晶型物，而且看来这些新的多晶型物都是不同的。通过减少阶段数来改进过程的方法通常具有成本效益，但会导致处理问题。例如，制备吩噻嗪烷基磺酸酯衍生物的一步法使用了非常有效的致癌磺酸内酯化合物。专利中描述了一种纯化罗宾尼罗（一种用于治疗帕金森氏症的药物）的方法，该专利确实消除了有害和有毒试剂的使用。该专利描述了一种去除有色杂质的方法，但是不清楚实际使用哪种试剂，因此本发明的基础是什么。描述了一种避免使用可能不稳定的重氮盐的制备高纯度氟异喹啉盐的方法。有机溶剂的去除或最小化是一个活跃的领域，并且制备咪唑-2-硫酮的方法不使用溶剂，并且通常从液体试剂开始。在不可能或产物为固体的情况下，将熔点降低剂加入反应混合物中，产物收率非常好。产生香气化学异胡薄荷醇的富集混合物的方法使用熔融结晶技术，该技术也避免使用溶剂。用于制备噻唑农药的中间体的纯化通常通过蒸馏进行，但某些反应杂质可能会形成共沸物。通过在蒸馏之前除去这些物质，可以改善工艺。离子液体作为试剂和溶剂是令人感兴趣的，一种新方法声称可以生产出几乎任何阴离子且杂质含量非常低的此类化合物。羟考酮用于缓解手术后的剧烈疼痛，两项专利描述了去除药物中迈克尔受体杂质水平的方法。在这两个过程中确实存在一些重叠，这可能会导致当事方之间的法律纠纷。卤化反应会引起废物处理或安全问题，两项专利解决了这些问题。一种在吡唑类抗抑郁药的合成过程中，在碘化步骤中用F5C5I代替1,2-二碘乙烷，另一种通过使用AlBr3和Br2改善了二溴二金刚烷的生产。在两个单独的专利中，描述了用于制备抗精神病药物喹硫平和阿塞那平的新方法。描述了一系列苯并咪唑化合物的糖衍生物，它们是抗病毒药，并且公开了制备包括新型中间体的止吐药dolasteron的新途径。此系列中的许多专利都描述了以公斤或几千公斤规模进行的实验，这可能暗示了。发展甚至通讯的高级阶段

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