甲烷氧化还原酶辅酶因子420(F 420)的第一个全合成是通过在受保护的10- D -ribityl-8-羟基-5-deazaisoalloxazine部分和一个肽部分之间形成一个磷酸三酯键来实现的(L-乳酸-γ- L-谷氨酰基)-L-谷氨酸三苄基酯,通过亚磷酸三酯方法,使用β,β,β-三氯乙基二氯亚磷酸酯,随后连续脱保护。
benzylidene moiety and the biological activity of these chiral compounds were studied. Structural studies show that compound with higher hydrogen bonding interactions show higher antibacterial activity. The results show chiral hydrazone derivatives based on lactic acid hydrazide could be used as potential lead compounds for developing novel antibacterialagents.
摘要 通过(S)-乳酸酰肼与水杨醛衍生物缩合合成了一系列新型手性乳酸腙衍生物,并通过元素分析和光谱研究(FT-IR、1H NMR和13C NMR光谱)进行了表征。一种化合物的结构是通过单晶 X 射线分析确定的。通过肉汤微量稀释法研究合成的化合物对作为细菌培养物的金黄色葡萄球菌、肺炎链球菌、大肠杆菌和铜绿假单胞菌的抗菌活性。所有合成的化合物均显示出良好的抗菌活性,MIC 范围为 64-512 μg/mL。化合物(S,E)-2-羟基-N-(2-羟基-5-硝基亚苄基)丙酰肼(5)和(S,
Accessing water processable cyanido bridged chiral heterobimetallic Co(<scp>ii</scp>)–Fe(<scp>iii</scp>) one dimensional network
A water processable cyanido bridged extended chiral heterobimetallic Co(II)–Fe(III) network is assembled. The unusual water processability of the coordinationpolymer originates from dangling hydrophilic substituents. The present approach offers a simple route to impart solution processability to cyanido bridged molecular magnetic materials.
[EN] FGFR3 INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS DE FGFR3
申请人:LILLY CO ELI
公开号:WO2022187443A1
公开(公告)日:2022-09-09
The present invention provides compounds of the formula:, for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.
Stable Amide Activation of <i>N</i>-Acetylated Glycosamines for the Synthesis of Fused Polycyclic Glycomimetics
作者:Samaneh Zarei、Mélina Motard、Samy Cecioni
DOI:10.1021/acs.orglett.3c03803
日期:2024.1.12
underexplored target for chemoselective derivatization and generation of glycomimetic scaffolds. Through mild amide activation, we report that N-acetimidoyl heterocycles are stable in neutral or basic conditions yet are excellent leavinggroups through acid catalysis. While this specific reactivity could prove broadly useful in amide activation strategies, stably activated N-acetylated sugars can also be diversified
碳水化合物的N-乙酰化是化学选择性衍生化和糖模拟支架生成的一个尚未充分探索的靶标。通过温和的酰胺活化,我们报告N-乙酰亚氨基杂环在中性或碱性条件下是稳定的,并且通过酸催化是优异的离去基团。虽然这种特定的反应性可能在酰胺活化策略中广泛有用,但也可以使用酰肼库使稳定活化的N-乙酰化糖多样化。我们优化了酸催化的一锅法序列,包括亲核置换、环脱水和分子内糖基化,最终产生与吗啉或哌嗪融合的吡喃糖苷。这种稳定激活后进行酸触发反应序列的策略例证了富含 3D 的融合糖模拟文库的有效组装。
Kimachi, Tetsutaro; Tanaka, Kiyoshi; Yoneda, Fumio, Journal of Heterocyclic Chemistry, 1991, vol. 28, # 2, p. 439 - 443