1-Azido-2-(methoxymethoxy)ethane 、 2-[(4-Bromophenyl)methyl]-3-methyl-1,1-dioxo-5-prop-2-ynyl-1,2,5-thiadiazepan-4-one 在
CuI immobilized on Amberlyst-21 作用下,
以
二氯甲烷 为溶剂,
反应 14.0h,
生成 C19H26BrN5O5S
参考文献:
名称:
Automated Synthesis of a 184-Member Library of Thiadiazepan-1,1-dioxide-4-ones
摘要:
The construction of a 225-member (3 x 5 x 15) library of thiadiazepan-1,1-dioxide-4-ones was performed on a Chemspeed Accelerator (SLT-100) automated parallel synthesis platform, culminating in the successful preparation of 184/225 sultams. Three sultam core scaffolds were prepared based upon the e utilization of an aza-Michael reaction on a multifunctional vinyl sulfonamide linchpin. The library exploits peripheral diversity in the form of a sequential, two-step [3 + 2] Huisgen cycloaddition/Pd-catalyzed Suzuki-Miyaura coupling sequence.
Automated Synthesis of a 184-Member Library of Thiadiazepan-1,1-dioxide-4-ones
作者:Erik Fenster、Toby R. Long、Qin Zang、David Hill、Benjamin Neuenswander、Gerald H. Lushington、Aihua Zhou、Conrad Santini、Paul R. Hanson
DOI:10.1021/co100060x
日期:2011.5.9
The construction of a 225-member (3 x 5 x 15) library of thiadiazepan-1,1-dioxide-4-ones was performed on a Chemspeed Accelerator (SLT-100) automated parallel synthesis platform, culminating in the successful preparation of 184/225 sultams. Three sultam core scaffolds were prepared based upon the e utilization of an aza-Michael reaction on a multifunctional vinyl sulfonamide linchpin. The library exploits peripheral diversity in the form of a sequential, two-step [3 + 2] Huisgen cycloaddition/Pd-catalyzed Suzuki-Miyaura coupling sequence.