Hexamethyldisilazane-Mediated Amidination of Sulfonamides and Amines with Formamides.

Hexamethyldisilazane was reacted with formamides to generate N,N-disubstituent formimidamide, after which a reaction with sulfonamides was induced to form sulfonylformamidines. This protocol can be applied for arylformamidine formation in which anilines are used as substrates under optimized conditions. The advantages of this method are high efficiency, structural diversity in products with good yields, and applicability in large-scale operations.

A facile access to N-sulfonylthioimidates and their use for the transformation to 3,4-dihydroquinazolines.

N-Sulfonylthioimidates can be efficiently synthesized through one-pot three-component coupling of terminal alkynes, sulfonyl azides, and thiols by using a copper(i) catalyst in the presence of 4-dimethylaminopyridine. The proposed reaction is characterized by mild reaction conditions and tolerance of diverse functional groups. Additionally, the crucial pharmacophore of 3,4-dihydroquinazolines was synthesized using a one-pot synthetic strategy from N-sulfonylthioimidates.

Facile access to N-formyl imide as an N-formylating agent for the direct synthesis of N-formamides, benzimidazoles and quinazolinones.

N-Formamide synthesis using N-formyl imide with primary and secondary amines with catalytic amounts of p-toluenesulfonic acid monohydrate (TsOH·H2O) is described. This reaction is performed in water without the use of surfactants. Moreover, N-formyl imide is efficiently synthesized using acylamidines with TsOH·H2O in water. In addition, N-formyl imide was successfully used as a carbonyl source in the synthesis of benzimidazole and quinazolinone derivatives. Notable features of N-formylation of amines by using N-formyl imide include operational simplicity, oxidant- and metal-free conditions, structurally diverse products, and easy applicability to gram-scale operation.

Research progress of three long-acting basic insulin analogues / 药物评价研究

Diabetes is a kind of worldwide chronic disease with high incidence,which threatens people's lives and work.With the development of DNA recombination technology,long-acting basal insulin analogues bring gospel and hope for patients with diabetes.Insulin glargine (IGla),detemir (IDet) and degludec (IDeg),as three basic types of insulin,commonly used in clinical practice that slowly absorbed and distributed by changing the structure,and relatively long acting time,more fit the physiological model of insulin secretion.Therefore,the existing studies of molecular structure,long-acting mechanism,safety evaluation and pharmacodynamic effects of three kinds of insulin preparations are briefly summarized.