丙酮 、 一水合肼 、 3,3-diethoxy-1,2-bis(2-pyridinyl)-1-propanone 在
acetone hexane 作用下,
以
乙醇 为溶剂,
反应 1.0h,
以to yield about 4 g of 4,5-bis(2-pyridinyl)-1H-pyrazole as a light tan solid的产率得到4,5-bis(2-pyridinyl)-1H-pyrazole
参考文献:
名称:
Pyridinyl-1H-pyrazole-1-alkanamides as antiarrhythmic agents
Azole-1-alkanamides as antiarrhytmic agents and preparation thereof
申请人:STERLING DRUG INC.
公开号:EP0388691A1
公开(公告)日:1990-09-26
N-[(alkylkamino)alkyl]-4,5-diaryl-1H-pyrazole-1-acetamides of formula
or acid-addition salt thereof wherein R¹ is hydrogen or lower-alkyl; R² and R³ are independently hydrogen, lower-alkyl, or hydroxy lower-alkyl, or R² and R³ together form a straight or branched alkylene chain of four to six carbons; A is CH₂CH(OH)CH₂ or (CH₂)n wherein n is an integer from two to eight; Ar¹ and Ar² are independently pyridinyl, phenyl, or phenyl substituted with methoxy, hydroxy or halogen; and at least one of Ar¹ and Ar² is pyridinyl, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.