创新催化剂生产药物应用的n -苄基苯胺

A. Alshammari, Rashid M. Altamimi, Rajenahally V. Jagadeesh
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引用次数: 0

摘要

促进药品关键成分高效生产的创新在制药行业被认为对产品的成本、功效和质量有相当大的好处,从而提高最终用户的满意度。我们报告了n -苄基苯胺(NBA)的权宜生产,这无疑表明了它对生产几种呼吸系统疾病(如哮喘、慢性、肺癌、肺结核等)药物的极端重要性。目前,NBA的制作是一个复杂而昂贵的过程。NBA的合成依赖于许多原材料,涉及许多步骤,这对最终产品的价格产生了不利影响。因此,通过开发新型材料,将NBA的复杂性和成本降至最低,从而获得的潜在收益是值得追求的。因此,本研究涉及开发新型钯催化剂,以一步法获得NBA。各种简单的和取代的芳族胺、杂环胺和脂肪族胺与苯甲醇反应,得到相应的n -苄基化胺,收率可达95%。值得注意的是,所获得的pd催化剂制备已扩大到公斤级,并且小(mg和g)和大(kg)制备的催化剂具有相似的结构特征和活性。
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Innovative Catalyst to Produce N-Benzylaniline for Drug Applications
Innovations that promote the efficient manufacture of the key ingredients in drugs are recognised in the pharmaceutical industry as conferring considerable benefits to the cost, efficacy and quality of products, thereby raising the satisfaction of the end users. We report the expedient production of N-benzylaniline (NBA) which undoubtedly demonstrates its extreme importance to manufacture several drugs for respiratory diseases (e.g. asthma, chronic, lung cancers, tuberculosis, etc.). Presently, the production of NBA is a complicated and costly process. The synthesis of NBA is dependent upon a number of raw materials and involves many steps, which adversely affects the price of the end product. Therefore, the potential gains that can be attained by developing novel materials that minimise the complexity and expense of NBA are worthy of pursuit. Therefore, the present study involves the development of novel Pd catalyst to obtain NBA in single step process. Various simple and substituted aromatic, heterocyclic and aliphatic amines were reacted with benzyl alcohol to produce their corresponding N-benzylated amines in good to excellent yields (up to 95% Yield of NBA). Noteworthy, obtained Pd-catalyst preparation has been up-scaled to kilogram scale and catalysts prepared in both small (mg and grams) and large-scale (kilograms) exhibited similar structural features and activity.
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