Acid-Free Silver-Catalyzed Cross-Dehydrogenative Carbamoylation of Pyridines with Formamides
作者:Wei Han、Fengli Jin、Qian Zhao、Hongyan Du、Lifang Yao
DOI:10.1055/s-0035-1561975
日期:——
have the apparent advantages over N-protected derivatives as synthetic building blocks. However, no practical methods have been developed for direct synthesis of this compound class from unfunctionalized pyridines. We herein present a general, safe, concise, acid-free, and highly selective method for the C2-carbamoylation of pyridines with unprotected formamide and N-methyl formamide through the cleavage
主要的吡啶基甲酰胺是生物活性分子中普遍存在的母体结构,与作为合成结构单元的 N 保护衍生物相比具有明显的优势。然而,尚未开发出从非官能化吡啶直接合成此类化合物的实用方法。我们在此提出了一种通用、安全、简洁、无酸和高选择性的方法,用于通过裂解两个 C-H 键,用未保护的甲酰胺和 N-甲基甲酰胺对吡啶进行 C2-氨基甲酰化。
The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
New thiazole derivatives, processes for the preparation thereof and pharmaceutical compositon comprising the same
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0417751A2
公开(公告)日:1991-03-20
A compound of the formula :
wherein R' is amino which may have suitable substituent ( s). hydroxy. halogen, cyano, acyl, heterocyclic thio, heterocyclic group or a group of the formula :
in which R4 is hydrogen, cyano or acyl. and
R5 is amino or lower alkoxy.
R2 and R3 are each hydrogen, acyl or lower alkyl which may have halogen: or
R2 and R3 are linked together to form lower alkylene.
in which R6 is hydrogen or halogen, and
A is bond or lower alkylene,
provided that
when R1 is amino which may have suitable substituent(s) and
A is bond; or R1 is lower alkylthioureido
and A is lower alkylene, then
and pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions comprising them as an active. ingredient.
式中的化合物
其中 R'为氨基,可具有合适的取代基(s)、羟基、卤素、氰基、酰基、杂环硫基、杂环基团或式......的基团:
其中 R4 是氢、氰基或酰基。
R5 是氨基或低级烷氧基。
R2 和 R3 各为氢、酰基或低级烷基,其中可含卤素:或
R2 和 R3 连接在一起形成低级亚烷基。
其中 R6 是氢或卤素,以及
A 是键或低级亚烷基、
条件是
当 R1 是氨基,可有适当的取代基,且
A 为键;或 R1 为低级烷基硫脲基,且 A 为低级亚烷基时
且 A 为低级亚烷基,则
以及它们的药学上可接受的盐、它们的制备方法和含有它们作为活性成分的药物组合物。