Chemistry and hypoglycemic activity of benzimidoylpyrazoles
作者:James R. Shroff、Victor Bandurco、Rohit Desai、Sidney Kobrin、Peter Cervoni
DOI:10.1021/jm00144a031
日期:1981.12
(tolazamide, phenformin, and buformin) in several experimental models show that these compounds seem to combine in one molecule some of the biological activities of the beta-cytotrophic sulfonylureas and some of the activities of the biguanides. A synthetic scheme for the preparation of the benzimidolypyrazoles and a preliminary structure-activity relationship are presented.
BF<sub>3</sub>-Promoted Ring Expansion of Iminylphosphiranes and Acylphosphiranes for Divergent Access to 1,2-Azaphospholidines and 1,2-Dihydrophosphetes
作者:Mingyue Cui、Yang Xu、Rongqiang Tian、Zheng Duan
DOI:10.1021/acs.orglett.3c04347
日期:2024.3.8
Ringexpansion of strained smallrings provides an efficient method for the synthesis of various high-value carbocycles and heterocycles. Here we report BF3·Et2O as both an activating reagent and fluorine source, enabling ringexpansion of phosphirane and P–F bond formation. Treatment of 1-iminylphosphirane complexes with BF3·Et2O resulted in 1,2-azaphospholidines, while the reaction of 1-acylphosphirane
应变小环的扩环为合成各种高价值碳环和杂环提供了一种有效的方法。在这里,我们报告BF 3 ·Et 2 O既作为活化剂又作为氟源,使得磷杂环扩环并形成P-F键。用BF 3 ·Et 2 O处理1-亚氨基正膦配合物得到1,2-氮杂磷烷,而1-酰基正膦配合物与BF 3 ·Et 2 O反应得到1,2-二氢磷酸酯。通过 N 和 O 原子对中间体鏻阳离子的亲核性来调整反应路径。
Direct acylamination of pyridine 1-oxide with N-phenylarenimidoyl chlorides and fluorides
作者:Rudolph A. Abramovitch、Jacek Pilski、Antoni Konitz、Piotr Tomasik
DOI:10.1021/jo00171a048
日期:1983.11
Innovative Strategy toward Mutant CFTR Rescue in Cystic Fibrosis: Design and Synthesis of Thiadiazole Inhibitors of the E3 Ligase RNF5