Van Den Hauwe, Robin; Elsocht, Mathias; Hollanders, Charlie; Ballet, Steven published their research in Synlett in 2021. The article was titled 《Efficient synthesis of polysubstituted 1,5-benzodiazepinone dipeptide mimetics via an Ugi-4CR-Ullmann condensation sequence》.Category: iodides-buliding-blocks The article contains the following contents:
An efficient three-step synthesis towards 3-amino-1,4-benzodiazepin-2-one derivatives is presented. The versatile Ugi-4-component reaction (Ugi-4CR) and Boc deprotection is followed by a ligand-free Ullmann condensation. This protocol allows the rapid construction of a diverse array of substituted 1,5-benzodiazepinones. Since Ugi-based products are typically limited by their ‘inert’ C-terminal amides, the use of a convertible (‘cleavable’) isocyanide was envisaged and resulted in building blocks that can be made SPPS compatible. To demonstrate the potential of this novel synthetic route, the design and preparation of novel phenylurea-1,5-benzodiazepin-4(5 H)-one dipeptide mimetics with potential CCK2-antagonist properties is reported. In the experiment, the researchers used many compounds, for example, 4-Chloro-2-iodoaniline(cas: 63069-48-7Category: iodides-buliding-blocks)
4-Chloro-2-iodoaniline(cas: 63069-48-7) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com