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Efficient procedure of mono, Di and Tri substituted amidines from amides using AlMe3
( Shanmugavel Ramachandran ),이상협 한국공업화학회 2015 한국공업화학회 연구논문 초록집 Vol.2015 No.1
Organo-aluminum motifs are more significant reagents due to their low cost, high selectivity and considerable stabilities. Owing to these advantages of organo-aluminum moiety, it has been applied in various organic transformations. Traditionally, garigipati introduced AlMe3 in the synthesis of unsubtititued amidines from nitriles and later by many others. We herein report the simple procedure for synthesis of mono, di and tri substituted amidines from primary, secondary and tertiary amides.
( Shanmugavel Ramachandran ),이상협 한국공업화학회 2014 한국공업화학회 연구논문 초록집 Vol.2014 No.1
Quinoxaline derivatives exhibit a wide range of biological functions including various antibiotics such as Echinomycin, Levomycin and Actinoleutin that are known to inhibit growth of gram positive bacteria and are active against various transplantable tumours. Initially, ethyl 2-(2-azidophenylamino)-2-oxoacetate, which was previously obtained from the coupling reaction between ethyl 2-chloro-2-oxoacetate and azidoaniline was subjected to N-alkylation with various alkylating agents in presence of LiHMDS. Then, these alkylated products were cyclized by the treatment of TPP to yield corresponding 3-amino-1-quinoxalin- 2 (1H)-ones via Staudinger reaction followed by aza-Wittig reaction, which can be finally derivatized by Lewis acid mediated smart cleavage.