Abstract：
A lot of advancement has been made in the area of β-lactams in recent times. Most of the research is targeted towards the synthesis of novel β-lactams, their functionalization and exploring their biological potential. The C-3 functionalization of β-lactams has continued to attract considerable interest of the scientific community due to their utility as versatile intermediates in organic synthesis and their therapeutic applications. This has led to the significant increase in efforts towards developing efficient and economic strategies for C-3 functionalized β-lactams.
The present review aims to highlight recent advancement made in C-3 functionalization of β - lactams.
To summarize, functionalization of β-lactams at C-3 is an essential aspect of β-lactam chemistry in order to improve/modify its synthetic utility as well as biological potential. The C-3 carbocation equivalent method has emerged as an important and convenient strategy for C-3 functionalization of β-lactam heterocycles which provides a wide range of β-lactams viz. 3-alkylated β-lactams, 3-aryl/heteroarylated β-lactams, 3- alkoxylated β-lactams. On the other hand, base mediated functionalization of β-lactams via carbanion intermediate is another useful approach but their scope is limited by the requirement of stringent reaction conditions. In addition to this, organometallic reagent mediated α-alkylation of 3-halo/3-keto-β-lactams also emerged as interesting methods for the synthesis of functionalized β-lactams having good yields and diastereoselectivities.
The present review aims to highlight recent advancement made in C-3 functionalization of β - lactams.
To summarize, functionalization of β-lactams at C-3 is an essential aspect of β-lactam chemistry in order to improve/modify its synthetic utility as well as biological potential. The C-3 carbocation equivalent method has emerged as an important and convenient strategy for C-3 functionalization of β-lactam heterocycles which provides a wide range of β-lactams viz. 3-alkylated β-lactams, 3-aryl/heteroarylated β-lactams, 3- alkoxylated β-lactams. On the other hand, base mediated functionalization of β-lactams via carbanion intermediate is another useful approach but their scope is limited by the requirement of stringent reaction conditions. In addition to this, organometallic reagent mediated α-alkylation of 3-halo/3-keto-β-lactams also emerged as interesting methods for the synthesis of functionalized β-lactams having good yields and diastereoselectivities.
摘要：
近年来,β-内酰胺领域取得了很大进展。大多数研究都是针对新型β-内酰胺的合成，它们的功能化和探索它们的生物潜力。β-内酰胺的C-3官能化由于它们作为有机合成中的通用中间体及其治疗应用的实用性而继续引起科学界的极大兴趣。这导致了开发C-3官能化β-内酰胺的有效和经济策略的努力的显著增加。
本综述旨在强调β-内酰胺的C-3官能化的最新进展。
总结一下，β-内酰胺在C-3的官能化是β-内酰胺化学的一个重要方面，以改善/改变其合成效用以及生物潜力。C-3碳阳离子当量方法已成为β-内酰胺杂环的C-3官能化的重要而方便的策略，该方法提供了广泛的β-内酰胺。3-烷基化β-内酰胺，3-芳基/杂芳基化β-内酰胺，3-烷氧基化β-内酰胺。另一方面,通过碳负离子中间体对β-内酰胺进行碱介导的官能化是另一种有用的方法,但是它们的范围受到严格反应条件要求的限制。除此之外,有机金属试剂介导的3-卤代/3-酮-β-内酰胺的α-烷基化也成为合成具有良好收率和非对映选择性的官能化β-内酰胺的令人感兴趣的方法。
本综述旨在强调β-内酰胺的C-3官能化的最新进展。
总结一下，β-内酰胺在C-3的官能化是β-内酰胺化学的一个重要方面，以改善/改变其合成效用以及生物潜力。C-3碳阳离子当量方法已成为β-内酰胺杂环的C-3官能化的重要而方便的策略，该方法提供了广泛的β-内酰胺。3-烷基化β-内酰胺，3-芳基/杂芳基化β-内酰胺，3-烷氧基化β-内酰胺。另一方面,通过碳负离子中间体对β-内酰胺进行碱介导的官能化是另一种有用的方法,但是它们的范围受到严格反应条件要求的限制。除此之外,有机金属试剂介导的3-卤代/3-酮-β-内酰胺的α-烷基化也成为合成具有良好收率和非对映选择性的官能化β-内酰胺的令人感兴趣的方法。
