tailieunhanh - Lithiation of 2-bromo-4-(1,3-dioxolan-2-yl)-1,3-thiazole

The reaction of lithiation of 2-bromo-4-(1,3-dioxolan-2-yl)-1,3-thiazole with in position 5 of the thiazole ring and double lithiation with t-butyllithium (t-BuLi) in positions 2 and 5 lithium diisopropylamide (LDA) are investigated. | Lithiation of 2-bromo-4- 1 3-dioxolan-2-yl -1 3-thiazole Current Chemistry Letters 7 2018 1 8 Contents lists available at GrowingScience Current Chemistry Letters homepage Lithiation of 2-bromo-4- 1 3-dioxolan-2-yl -1 3-thiazole Vitaliy O. Sinenko Sergiy R. Slivchuk and Volodymyr S. Brovarets Institute of Bioorganic Chemistry and Petrochemistry National Academy of Sciences of Ukraine Murmanska str. 1 02094 Kyiv Ukraine CHRONICLE ABSTRACT Article history The reaction of lithiation of 2-bromo-4- 1 3-dioxolan-2-yl -1 3-thiazole with in position 5 of Received December 22 2017 the thiazole ring and double lithiation with t-butyllithium t-BuLi in positions 2 and 5 lithium Received in revised form diisopropylamide LDA are investigated. When lithiated and dilithiated thiazoles were treated January 29 2018 with different electrophiles a number of trifunctional 1 3-thiazoles were obtained with high Accepted January 30 2018 yields. Available online January 30 2018 Keywords 1 3-thiazole 2-bromo-4- 1 3-dioxolan-2-yl - 1 3-thiazole Lithiation Lithium diisopropylamide T-butyllithium 2018 Growing Science Ltd. All rights reserved. 1. Introduction Natural and synthetic derivatives of 1 3-thiazole have diverse biological activity and play a significant role in the processes of life which stimulates a steady interest in research in the synthesis of new derivatives of this type. 1 3-Thiazole derivatives exhibit the activities of selective enzyme inhibitors 1-4 sigma receptors 5 6 adenosine receptors7 8 antagonists and new T-type calcium channel The actual task today is to obtain polyfunctional 1 3-thiazoles which are suitable for further modification in order to synthesize the libraries of thiazole derivatives for screening and searching for pharmacologically promising compounds. One of the methods of such products synthesis calls for metalation reagents giving with 1 3-thiazoles organometallic derivatives which are converted into functionalized 1 .

• Hoá học
• 1 3 thiazole
• 5 lithium diisopropylamide
• Lithiated and dilithiated thiazole
• Diverse biological activity
• T type calcium channel blocker