Metal-Free Aminothiation of Alkynes: Three-Component Tandem Annulation toward Indolizine Thiones from 2-Alkylpyridines, Ynals, and Elemental Sulfur
作者:Zhengwang Chen、Pei Liang、Fan Xu、Zhen Deng、Lipeng Long、Guotian Luo、Min Ye
DOI:10.1021/acs.joc.9b01802
日期:2019.10.4
A metal-free three-component annulation reaction for the synthesis of indolizine thiones via tandem C-C/C-N/C-S bondformation was developed. Various 2-alkylpyridines with aromatic ynals and elemental sulfur proceeded smoothly under catalyst-free conditions, and the desired products were obtained in moderate to excellent yields.
catalyzed synthesis of indolizine-1-carboxylates through oxidative CC and CN bondformations by the reaction of 2-pyridyl acetates with alkynes and alkenes without metal, oxidant, and base. This procedure is compatible with a broad range of functional groups in both alkynes and alkenes with good yields. The reaction proceeds through a tandem CC bondformation followed by an intramolecular cyclization
Copper-catalyzedsynthesis of imidazo[1,5-a]pyridine-1-carboxylates through oxidative amination of C(sp3)–H bonds under mild aerobic conditions with broad substrate scope is described. Use of naturally abundant air as the sole oxidant was found to be efficient and selective. The present protocol is also applicable for direct synthesis of functionalized imidazo[1,5-a]pyridines from amino acid derivatives
铜催化的咪唑并[1,5 - a ]吡啶-1-羧酸铜的合成在温和的好氧条件下通过广泛的底物范围内的C(sp 3)-H键的氧化胺化进行了描述。发现使用自然丰富的空气作为唯一氧化剂是有效和选择性的。本协议也适用于从氨基酸衍生物直接合成功能化的咪唑并[1,5- a ]吡啶。
Copper-mediated synthesis of pyrazolo[1,5-a]pyridines through oxidative linkage of C–C/N–N bonds
Copper-mediated synthesis of pyrazolo[1,5-a]pyridine-3-carboxylates through oxidative linkage of C–C and N–N bonds under mild reaction conditions with broad substrate scope is described.
Design, synthesis and cytotoxicity studies of novel pyrazolo[1, 5-a]pyridine derivatives
作者:Chitrakar Ravi、Arem Qayum、Darapaneni Chandra Mohan、Shashank K. Singh、Subbarayappa Adimurthy
DOI:10.1016/j.ejmech.2016.11.037
日期:2017.1
Copper–mediated synthesis of various pyrazolo[1, 5–a]pyridine-3-carboxylates has been described. The biological activities of these molecules have been evaluated against various human cancer cell lines A549 (Lung adenocarcinoma cell line), MCF-7 (Breast carcinoma cell line), HCT-116 (Colon cancer cell line), and PC-3 (Prostate cancer cell line) through SRB assay. Compound 247 led to accumulation MCF-7 cells