TiCl<sub>4</sub> mediated facile synthesis of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles
作者:Lin Zhang、Yu Yu、Qiang Tang、Jianyong Yuan、Dongzhi Ran、Binghua Tian、Tao Pan、Zongjie Gan
DOI:10.1080/00397911.2019.1700521
日期:2020.2.1
Abstract An efficient method for the synthesis of 2,5-disubstituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles has been developed. Various hydrazides or thionyl hydrazides readily react with DMA derivatives in the presence of TiCl4 as a catalyst to afford the desired products. This protocol provides a simple and economical procedure that affords the target products with good yields and wide substrate
[EN] DIMERIC COMPOUNDS AS STING AGONISTS<br/>[FR] COMPOSÉS DIMÈRES UTILISÉS EN TANT QU'AGONISTES DE STING
申请人:MERSANA THERAPEUTICS INC
公开号:WO2021113679A1
公开(公告)日:2021-06-10
The present disclosure relates to dimeric STING agonists of Formulae (I), (II), (III), (IV), (V), and (VI), and pharmaceutically acceptable salts thereof. The present disclosure also relates to methods of preparing the compounds and methods of using the compounds.
A method for producing a β-alkoxypropionamide including reacting a β-alkoxypropionic acid ester represented by the following formula (1) and an amine represented by the following formula (2) in the presence of a polyol and a basic catalyst, thereby to produce a β-alkoxypropionamide represented by the following formula (3),
wherein, as the polyol, a reaction residue that is generated by the reaction and contains a used polyol is used: (wherein in the formulas, R and R' are independently a C1 to C6 linear, branched or cyclic, saturated hydrocarbon group; R1 and R2 are independently a C1 to C6 linear, branched or cyclic, saturated hydrocarbon group; and R3 is H or CH3).