developed a new synthetic method for monodehydro-2,5-diketopiperazines (monodehydroDKPs), which is based on an acid catalyzed cyclization of N-α-ketoacyl aminoacidamides. Using this cyclization reaction, monodehydroDKP was formed with no or slight racemization in case that N-α-ketoacyl aminoacidamides with β-aliphatic-α-ketoacyl groups and sterically unhindered N-substituting groups at the C-terminal amide
[EN] PURINE DERIVATIVES AS CD73 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE PURINE EN TANT QU'INHIBITEURS DE CD73 POUR LE TRAITEMENT DU CANCER
申请人:VITAE PHARMACEUTICALS INC
公开号:WO2015164573A1
公开(公告)日:2015-10-29
Provided are novel compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
New Strategies to Cyclic <i>α</i>-Thiophosphonates
作者:Joel D. Moore、Kevin T. Sprott、Paul R. Hanson
DOI:10.1055/s-2001-13374
日期:——
A transition-metal-catalyzed approach to cyclic α-thiophosphonates is reported. This strategy incorporates both a Rh2(OAc)4-catalyzed [2,3]-sigmatropic rearrangement of intermediate sulfur-ylides generated from α-diazophosphonates and a ring-closing metathesis (RCM) of the resulting α-thiophosphonates 2 a - c to yield functionalized cyclic α-thiophosphonates 4 a - c.
报告了一种过渡金属催化的环状δ±-硫代磷酸酯的方法。该策略包括 Rh2(OAc)4 催化的δ-二氮膦酸盐生成的中间硫酰基的[2,3]-三向异性重排,以及由此生成的δ-硫代磷酸盐 2 a - c 的闭环偏析 (RCM),从而生成官能化的环状δ-硫代磷酸盐 4 a - c。
Novel furimazine derivatives for nanoluciferase bioluminescence with various C-6 and C-8 substituents
作者:Jie Li、Xiaoxu Wang、Gaopan Dong、Chongzheng Yan、Yuanyuan Cui、Zheng Zhang、Lupei Du、Minyong Li
DOI:10.1039/d1ob01098k
日期:——
Nanoluciferase (NLuc) is the emerging commercially available luciferase considering its small size and superior bioluminescence performance.