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酰氯类化合物(RCOCl,简称酰氯,下同)是化学合成中广泛应用的物质,化学性质较活泼,易起反应。在药物化学上,它们的用途可分为二个方面;首先是通过它而在羧基上引入某些基团,以制备新药物;其次,有一些低级酰氯,尤其是乙酰氯常作为酰化剂,用来保护某些如羟基及胺基等基团,以免在下一步反应中被破坏。但此种酰基常需在某一步骤除去。试以《机药物合成手册》收载的药物来统计,约有60个以上药物的合成,应用了酰氯类化合物,本文拟对酰氯的合成及其有关问题,作简略的讨论。
Acyl chloride compounds (RCOCl, hereinafter referred to as acid chloride, the same below) is widely used in chemical synthesis of substances, chemical properties more lively, easy to react. In medicinal chemistry, their use can be divided into two aspects; first, through the introduction of certain groups on the carboxyl group to prepare new drugs; Second, there are some lower acyl chloride, acetyl chloride is often used as acylating agent , Used to protect certain groups such as hydroxyl and amine, so as not to be destroyed in the next reaction. However, such acyl often need to be removed in one step. Try to “drug synthesis manual,” contained in the statistics to the drug, there are about 60 synthetic drugs, the use of acid chloride compounds, the synthesis of acid chloride and its related issues, a brief discussion.