Intramolecular cyclization strategies toward the synthesis of zoanthamine alkaloids
摘要:
Stabilized 2-amino-1,3-dienes can participate in intramolecular Diels-Alder (IMDA) reactions with pendant dienophiles. We found that these dienes can be readily prepared via standard palladium-mediated coupling reactions and have comparable reactivity to 2-oxodienes. Application of these substrates to the synthesis of tetracyclic model systems representing the ABCE motif of the zoanthamines is presented. (C) 2011 Elsevier Ltd. All rights reserved.
The versatile methodology was developed for synthesizing kujigamberol B, a dinorlabdane diterpenoid isolated from the methanol extract of Kuji amber. A highly efficient intramolecular cyclization is followed by a Sonogashira-coupling reaction during the total synthesis. The synthesized compounds were evaluated for the growth-restoring activity against the mutant yeast (zds1Δ erg3Δ pdr1Δ pdr3Δ) and
开发了用于合成 kujigamberol B 的多功能方法,kujigamberol B 是一种从 Kuji 琥珀的甲醇提取物中分离出来的二萘并萘烷二萜类化合物。在全合成过程中,高效的分子内环化之后是 Sonogashira 偶联反应。评估了合成化合物对突变酵母 (zds1Δ erg3Δ pdr1Δ pdr3Δ) 的生长恢复活性和 RBL-2H3 细胞的脱颗粒作用。我们发现在这两种活动中,伯醇和仲醇类似物与 kujigamberol B 一样活跃。
OREXIN RECEPTOR AGONISTS
申请人:[en]MERCK SHARP & DOHME LLC
公开号:WO2024107615A1
公开(公告)日:2024-05-23
The present invention is directed to compounds of Formula I which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.