A simple and efficient approach to realize difunctionalization of arylketones with malonate esters via electrochemical oxidation

2014 ◽  
Vol 50 (39) ◽  
pp. 5034-5036 ◽  
Author(s):  
Huihui Gao ◽  
Zhenggen Zha ◽  
Zhenlei Zhang ◽  
Huanyue Ma ◽  
Zhiyong Wang

A facile difunctionalization of arylketones with malonate esters via electrochemical oxidation was achieved under mild conditions.

Synthesis ◽  
2019 ◽  
Vol 52 (04) ◽  
pp. 609-618 ◽  
Author(s):  
Dianpeng Chen ◽  
Jianming Li ◽  
Yingying Shan ◽  
Peiying Cui ◽  
Yutong Zhao ◽  
...  

A novel halogen-radical-promoted dearomative aza-spiro­cyclization of alkynylimines for the synthesis of 3-halo-spirocyclohexadienones is described. In this process, it is believed that a radical addition, 5-exo-trig cyclization, and dearomative aza-spirocyclization are involved. Easily available starting materials, mild conditions, and a wide substrate scope make this approach potentially useful.


Synlett ◽  
2019 ◽  
Vol 30 (18) ◽  
pp. 2077-2080
Author(s):  
Wenxia Xie ◽  
Bowen Gong ◽  
Shulin Ning ◽  
Nian Liu ◽  
Zhuoqi Zhang ◽  
...  

A diethyl phosphite mediated electrochemical oxidation strategy for the synthesis of 3,4-dihydroisoquinolin-1(2H)-ones from tetrahydroisoquinolines under mild conditions has been developed. This protocol provides an environmentally friendly and simple way for the construction of C=O bonds in an undivided cell unit.


2020 ◽  
Vol 7 (18) ◽  
pp. 2612-2617
Author(s):  
Wenhao Dai ◽  
Chunpu Li ◽  
Yichu Liu ◽  
Xu Han ◽  
Xingjun Li ◽  
...  

An efficient approach to obtain saturated seven-membered ring containing three heteroatoms has been developed by using a palladium-catalyzed [4 + 3] dearomatizing cycloaddition. This approach features mild conditions and good functional group tolerance.


2017 ◽  
Vol 8 (9) ◽  
pp. 6419-6422 ◽  
Author(s):  
Wenchao Gao ◽  
Hui Lv ◽  
Tonghuan Zhang ◽  
Yuhong Yang ◽  
Lung Wa Chung ◽  
...  

The Ni-catalyzed asymmetric hydrogenation of challenging β-acylamino nitroolefins was achieved under mild conditions, affording β-acylamino nitroalkanes in excellent yields and with high enantioselectivities.


Synlett ◽  
2018 ◽  
Vol 29 (11) ◽  
pp. 1496-1501 ◽  
Author(s):  
J. Woollins ◽  
Guoxiong Hua ◽  
David Cordes ◽  
Alexandra Slawin

An efficient approach has been developed for the synthesis of new phosphorus–sulfur heterocycles by a one-pot three-component condensation reaction of a four-membered-ring thionation reagent [Lawesson’s reagent or its ferrocene analogue (2,4-diferrocenyl-1,3,2,4-diathiadiphosphetane 2,4-disulfide)], an alkane- or arenedithiol, and a dihaloalkane at room temperature in the presence of triethylamine. The simple synthesis method with mild conditions (room temperature and normal reactant concentrations) enhances further the application of the multicomponent reaction in the preparation of novel phosphorus–sulfur heterocycles. Six representative X-ray structures confirmed the formation of these macrocycles.


Synthesis ◽  
2019 ◽  
Vol 52 (02) ◽  
pp. 273-280 ◽  
Author(s):  
Fangran Liu ◽  
Xiaofei Zhang ◽  
Qun Qian ◽  
Chunhao Yang

Herein, a concise and efficient protocol to synthesize a series of 2,6-disubstituted 4-fluoropyrimidines as universal and useful building blocks in medicinal chemistry is reported. From readily accessible α-CF3 aryl ketones and different amidine hydrochlorides, this method provides a very practical approach to this kind of compounds under mild conditions with good to excellent yields.


Synthesis ◽  
2017 ◽  
Vol 50 (03) ◽  
pp. 555-564 ◽  
Author(s):  
Larisa Politanskaya ◽  
Evgeny Tretyakov

A simple and efficient approach to the synthesis of fluorinated amino-substituted acetophenones in good to excellent yields is reported. The heart of the proposed method consists of conversion of a Me3Si–C≡C– moiety into a MeC(=O)– group in the presence of p-tolu­ene­sulfonic acid (p-TSA) passing a stage of ethynylaniline formation. The reaction is metal-free, proceeds under mild conditions, and uses readily available starting compounds (trimethylsilylarylacetylene derivatives). The reaction provides access to amino-substituted acetophenones, which may serve as precursors for the synthesis of polyfluorinated azaheterocycles, having potential anticarcinogenic activity.


2017 ◽  
Vol 53 (50) ◽  
pp. 6792-6795 ◽  
Author(s):  
Qian Chen ◽  
Xiaoshuang Liu ◽  
Fang Guo ◽  
Zhonglin Chen

An unexpected rearrangement of pyrazolium halides was observed, presenting an efficient approach for the synthesis of 1,2-dihydroquinazolines under mild conditions.


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