Evidence for the Occurrence of Substitution Side Products in Grignard Reactions
摘要:
In the formation of Grignard reagents from 4-bromoalkoxybenzene and their subsequent coupling reactions with allylic halides, the unusual minor side products, 8 - 14 have been obtained.
KINASE INHIBITOR SCAFFOLDS AND METHODS FOR THEIR PREPARATION
申请人:Ding Sheng
公开号:US20070191380A1
公开(公告)日:2007-08-16
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
ANTIMICROBIAL POLYMYXINS FOR TREATMENT OF BACTERIAL INFECTIONS
申请人:MICURX PHARMACEUTICALS, INC.
公开号:US20160185823A1
公开(公告)日:2016-06-30
The present invention provides antimicrobial polymyxin compounds of the following formula I:
or pharmaceutically acceptable salts, hydrates, or solvates thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Potassium-base-mediated defluoroetherification of aryl and heteroaryl fluorides with alkoxyboronic acidpinacolesters under transition-metal-free conditions is reported. This protocol efficiently and safely provides a wide variety of aryl ethers in high yields without using metal catalysts, specific ligands, and harsh conditions to selectively forge Csp2–O bonds via the Csp2–F cleavage. This method
报道了在无过渡金属条件下,钾基介导的芳基和杂芳基氟化物与烷氧基硼酸频哪醇酯的脱氟醚化反应。该协议以高产率高效安全地提供多种芳基醚,无需使用金属催化剂、特定配体和苛刻条件,通过 C sp2 -F 裂解选择性地形成 C sp2 -O 键。该方法可应用于结构复杂的C sp2 -氟化物和生物活性醇如β-雌二醇、骨化醇和生育酚的后期醚化。
Iodotriphenylphosphonium iodide mediated deprotection of aryl alkyl ethers under metal-free and neutral conditions
A highly efficient method for the deprotection of arylalkylethers under metal-free and neutral conditions was developed by iodotriphenylphosphonium iodide [Ph3P+I]I− formed in situ through the reaction of equimolar PPh3 and I2. A variety of arylalkylethers including aryl methyl/allyl/benzyl/ethyl/n-propyl/i-propyl/n-butyl ethers can all be highly efficiently deprotected to release the corresponding
通过等摩尔 PPh 3和 I 2原位反应生成的碘化三苯基磷鎓 [Ph 3 P + I]I −开发了一种在无金属和中性条件下芳基烷基醚脱保护的高效方法。各种芳基烷基醚,包括芳基甲基/烯丙基/苄基/乙基/正丙基/异丙基/正丁基醚,都可以高效脱保护,以良好至优异的收率释放相应的酚类。