无溶剂条件下碘催化合成三吲哚甲烷的研究

室温无溶剂条件下,碘(5 mol%)催化吲哚与原甲酸三乙酯的反应,生成相应的三吲哚甲烷,产率适中到较好且无副产物。     

5-取代吲哚类化合物的合成

5－取代吲哚类化合物是一种重要的医药中间体。从古典的Fischer方法开始，有关合成5－取代吲哚类化合物的方法不断出现。本文对各种合成方法进行了介绍和评价。参考文献30篇。     

对甲苯磺酸催化三吲哚烷基化合物的合成

室温下,吲哚与3-吲哚甲醛在对甲苯磺酸的催化下高收率得到三吲哚烷基化合物,所有产物的结构经1H NMR,IR和HR-MS表征。     

磷钨酸催化合成双吲哚甲烷衍生物

磷钨酸;吲哚;亲电取代;双吲哚甲烷衍生物     

无溶剂条件下碘催化不对称双吲哚的合成

在室温以及无溶剂条件下,吲哚与烷基-3-吲哚基甲醇在碘的催化下以73％～99％的高收率得到不对称双吲哚烷基化合物。其结构经^1H NMR,IR及MS表征。     

新型螺环吡咯酮双氧化吲哚类化合物的无催化剂合成及其抗白血病活性

以3-异硫氰基氧化吲哚与3-丙二腈缩合的3-烯氧化吲哚为原料,乙腈为溶剂,在无催化剂存在的条件下于室温发生[3+2]环加成反应,合成了6个新型的螺环吡咯酮双氧化吲哚类化合物(3a~3f),产率91%~95%,dr 17/1~>20/1,其结构经¹H NMR, ¹³C NMR和HR-MS（ESI-TOF）表征。采用MTT法研究了3a~3f对人白血病细胞(K562)的体外抗肿瘤活性。结果表明：化合物3c对K562具有明显的抑制活性（IC₅₀为36.3 μM）,与阳性对照药顺铂接近。     

Eu(NTf2)3催化吲哚与醛(酮)反应合成二吲哚基甲烷

二(三氟甲基磺酰)亚胺铕(Ⅲ)[Eu(NTf2)3,Tf=SO2CF3]作催化剂,吲哚与醛(酮)在室温下发生亲电取代反应合成了一系列二吲哚基甲烷,产率85%～98%.该法反应条件温和、时间短、催化剂用量少且可以回收重复使用.     

新型3-吲哚-四取代氧化吲哚的无催化剂合成

以3-氯氧化吲哚为原料,在无催化剂条件下发生S_N1反应,合成了18个新型的3-吲哚-四取代氧化吲哚,产率34%~77%,其结构经¹H NMR, ¹³C NMR和HR-MS（ESI-TOF）表征。     

环状磷酸催化合成二吲哚甲烷衍生物

在环状磷酸催化下,通过吲哚和醛酮的亲电取代反应,室温下合成了一系列二吲哚甲烷衍生物.考察了催化剂结构、用量和溶剂等因素对反应的影响,确定了最优反应条件,提出了可能的反应机理.该方法具有操作简单、条件温和、催化剂用量少、产率高及环境友好等优点.     

Fischer吲哚合成法的研究进展

吲哚及其衍生物具有某些生物活性, 其合成方法很多. 其中Fischer吲哚合成是最便捷和经济的合成方法, 应用最多. 对此法近十年来的合成工艺进行了综述和评价.     

Highly Efficient Synthesis of Bis（indolyl）methanes Catalyzed by Sodium Tetrafluoroborate

Sodium tetrafluoroborate （NaBF4） was found to catalyze the electrophilic substitution reactions of indoles with aldehydes and ketones under solvent-free conditions to afford the corresponding bis（indolyl）methanes in high yields.     

Diammonium Hydrogen Phosphate as an Efficient and Inexpensive Catalyst for the Synthesis of Bis(indolyl)methanes under Solvent-Free Conditions

Summary. Bis(indolyl)methanes were synthesized by the reaction of indole derivatives and aromatic and aliphatic aldehydes in the presence of diammonium hydrogen phosphate as a solid catalyst under solvent-free conditions. This methodology offers significant improvements for the synthesis of bis(indolyl)methanes with regard to the yield of products, simplicity in operation, and green aspects by avoiding toxic catalysts and solvents.     

Hexamethylenetetraamine-Bromine Catalyzed Rapid and Efficient Synthesis of Bis(indolyl)methanes

Summary. Highly rapid and convenient syntheses of bis(indolyl)methanes in excellent yields were carried out using the inexpensive and easily available catalyst, hexamethylenetetraamine-bromine (HMTAB). Mild reaction conditions, short reaction times, and excellent yields are important features of this method.     

合成双吲哚甲烷类衍生物的研究进展

双吲哚甲烷类衍生物具有丰富的生物活性和药理活性,在医药领域得到了广泛的应用.近年来,对双吲哚甲烷类衍生物的合成研究引起了人们的热点关注.对双吲哚甲烷类衍生物的合成方法进行了综述,并将催化剂按照不同的类型分为:(1)路易斯酸催化剂,(2)分子碘催化剂,(3)质子酸催化剂,(4)固载催化剂,(5)杂多酸催化剂,(6)有机小分子催化剂,(7)配合物催化剂,(8)离子液体催化剂,(9)其它类型的催化剂.     

A Meldrum's Acid Catalyzed Synthesis of Bis(indolyl)methanes in Water under Ultrasonic Condition

A highly effective Meldrum's acid catalyzed synthesis of bis(indol‐3‐yl)methanes has been developed. This reaction provides the corresponding bis(indol‐3‐yl)methanes in high yields after short reaction time in the presence of 2 mol % catalyst in water under ultrasonic condition.     

无溶剂无催化条件下一锅合成芳酰基腈化合物

无溶剂无催化剂条件下,以芳香酸、二氯亚砜和铁氰化钾为原料,经氯化、氰化两步一锅合成了一系列芳酰基腈化合物。 考察了氰化过程中反应温度、反应时间对产率的影响。 实验结果表明,其最佳反应条件为：反应温度为180 ℃,反应时间为2 h,产物收率达71%~92%。 产物经IR、1H NMR和13C NMR分析确认。 本方法具有工艺操作简单、产率高、无溶剂无催化和环境友好等优点。     

Efficient Synthesis of Bis(heterocyclyl)methanes

The reaction of pyrrole/furan aldehyde with Grignard reagent and pyrrole/N-methyl pyrrole in sequence allows efficient synthesis of a number of meso-elaborated bis(heterocyclyl)methanes, which are otherwise difficult to obtain through a direct aldehyde condensation route.      

Diammonium Hydrogen Phosphate as an Efficient and Inexpensive Catalyst for the Synthesis of Bis(indolyl)methanes under Solvent-Free Conditions

Bis(indolyl)methanes were synthesized by the reaction of indole derivatives and aromatic and aliphatic aldehydes in the presence of diammonium hydrogen phosphate as a solid catalyst under solvent-free conditions. This methodology offers significant improvements for the synthesis of bis(indolyl)methanes with regard to the yield of products, simplicity in operation, and green aspects by avoiding toxic catalysts and solvents.     

Eu(NTf2)3催化吲哚与醛(酮)反应合成二吲哚基甲烷

二(三氟甲基磺酰)亚胺铕(III) [Eu(NTf₂)₃, Tf＝SO₂CF₃]作催化剂, 吲哚与醛(酮)在室温下发生亲电取代反应合成了一系列二吲哚基甲烷, 产率85%～98%. 该法反应条件温和、时间短、催化剂用量少且可以回收重复使用.     

First Synthesis of Bis(di(indolyl)aryl)methanes From Bis(salicylaldehydes)

In this article, a simple method for the synthesis of bis(di(indolyl)aryl)methanes is described. The iodine‐catalyzed (5 mol %) reaction of indoles with various bis(salicylaldehyde) derivatives affords the bis(di(indolyl)aryl)methanes in excellent yields. The reaction works well under mild reaction condition with shorter reaction time.