2-Aminopyridines via Reaction of Pyridine N-Oxides and Activated Isocyanides
摘要:
A practical and efficient method for the synthesis of substituted 2-aminopyridines from pyridine N-oxides is reported. Yields of purified, isolated products of up to 84% are observed for the one-pot, two-step process. The reaction involves an in situ deprotection of an isolable N-formylaminopyridine intermediate and facilitates the synthesis of 2-aminopyridines for which other methods fail.
Substituted amino-pyridine derivatives, processes for their preparation and pharmaceutical compositions containing them
申请人:BEECHAM GROUP PLC
公开号:EP0000816A1
公开(公告)日:1979-02-21
A class of substituted amino pyridine derivatives are of value in the treatment of diabetes. Some of the compounds also possess hypolipidaemic activity.
The compounds are represented by the formula (I):
wherein R3 is hydrogen, alkyl or an acidic function;
R2 is hydrogen or alkyl;
R4 and R' are hydrogen, alkyl or halogen;
Z is hydrogen, phenyl, alkyl or aralkyl;
Alk is alkylene and x is 0 or 1;
R1 is optionally substituted phenyl or naphthyl.
Most of the compounds of formula (I) are novel.
2-Aminopyridines via Reaction of Pyridine <i>N</i>-Oxides and Activated Isocyanides
作者:Mitchell Vamos、Nicholas D. P. Cosford
DOI:10.1021/jo402693s
日期:2014.3.7
A practical and efficient method for the synthesis of substituted 2-aminopyridines from pyridine N-oxides is reported. Yields of purified, isolated products of up to 84% are observed for the one-pot, two-step process. The reaction involves an in situ deprotection of an isolable N-formylaminopyridine intermediate and facilitates the synthesis of 2-aminopyridines for which other methods fail.
Hisano, Takuzo; Harano, Kazunobu; Matsuoka, Toshikazu, Chemical and pharmaceutical bulletin, 1985, vol. 33, # 5, p. 1869 - 1877