10592-27-5Relevant articles and documents
Iron-Catalyzed Amination of Strong Aliphatic C(sp3)-H Bonds
Das, Sandip Kumar,Roy, Satyajit,Khatua, Hillol,Chattopadhyay, Buddhadeb
, p. 16211 - 16217 (2020/10/26)
A concept for intramolecular denitrogenative C(sp3)-H amination of 1,2,3,4-tetrazoles bearing unactivated primary, secondary, and tertiary C-H bonds is discovered. This catalytic amination follows an unprecedented metalloradical activation mechanism. The utility of the method is showcased with the short synthesis of a bioactive molecule. Moreover, an initial effort has been embarked on for the enantioselective C(sp3)-H amination through the catalyst design. Collectively, this study underlines the development of C(sp3)-H bond functionalization chemistry that should find wide application in the context of drug discovery and natural product synthesis.
Synthesis method of 5-bromo-7-azaindole
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Paragraph 0043-0047; 0058-0063; 0075-0079, (2018/06/26)
The invention relates to a synthesis method of 5-bromo-7-azaindole. With 7-azaindole as a raw material, conjugation of the five-membered ring of indole is damaged by low-pressure liquid-phase hydrogenation, and a key medical intermediate 5-bromo-7-azaindole is prepared through oxybromination and nonmetal oxydehydrogenation. The product purity is higher than or equal to 99%. Bromine atoms are introduced by an oxybromination technology, the utilization rate of the bromine atoms exceeds 98%, the use of bromine is avoided, and the problem that a large amount of bromine-containing waste liquid is generated in original technology is solved. According to the synthesis method provided by the invention, through nonmetal catalytic dehydrogenation, heavy metal catalysis is avoided, the problem of heavy metal residue easily occurring in the product is solved, and the safety of medicine products is ensured. The reaction efficiency can be effectively improved, the reaction time is shortened, and thetotal reaction yield is increased; moreover, industrial waste liquid and residue is reduced, industrial popularization is facilitated, and remarkably high economic benefits are created.
Synthesis method of 5-chloro-7-azaindole
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, (2017/08/25)
The invention provides a synthesis method of 5-chloro-7-azaindole. The synthesis method comprises the following steps: (1) reacting a dilithium initiator and trimethylbromosilane to prepare silicon-containing organic lithium; (2) reacting 2-amino-3-methylpyridine and di-tert-butyl dicarbonate to prepare 2-N-BOC-amino-3-methylpyridine; (3) performing lithiation on the 2-N-BOC-amino-3-methylpyridine through the silicon-containing organic lithium, and performing delithiation activation, cyclization and dehydration to prepare 7-azaindole; (4) performing hydrogenation reduction reaction on the 7-azaindole to generate 2,3-dihydro-7-azaindole; (5) performing chlorination reaction on the 2,3-dihydro-7-azaindole through liquid chlorine to generate 5-chloro-2,3-dihydro-7-azaindole; and (6) performing dehydrogenation reaction on the 5-chloro-2,3-dihydro-7-azaindole to obtain 5-chloro-7-azaindole. The synthesis method provided by the invention has the advantages of mild conditions and high yield.