Facile Regiocontrolled Three-Step Synthesis of Poly-Substituted Furans, Pyrroles, and Thiophenes: Consecutive Michael Addition of Methyl Cyanoacetate to α,β-Enone, CuI-Mediated Aerobic Oxidation, and Acid-Catalyzed Paal-Knorr Synthesis
作者:Se-Hee Kim、Jin-Woo Lim、Cheol-Hee Lim、Jae-Nyoung Kim
DOI:10.5012/bkcs.2012.33.2.620
日期:2012.2.20
December 19, 2011An efficient synthesis of poly-substituted furans, pyrroles, and thiophenes was carried out in a regiocontrolledmanner via a three-step process; (i) conjugate addition of methyl cyanoacetate derivatives to α,β-enones, (ii)CuI-mediated aerobic oxidation, and (iii) Paal-Knorr type synthesis of five-membered heterocycles. Key Words : Furans, Pyrroles, Thiophenes, CuI, Paal-Knorr synthesisIntroductionRecently
E-mail: kimjn@chonnam.ac.kr 2011年12月6日接收,2011年12月19日接受 (i) 氰基乙酸甲酯衍生物与 α,β-烯酮的共轭加成,(ii) CuI 介导的有氧氧化,和 (iii) 五元杂环的 Paal-Knorr 型合成。关键词:呋喃,吡咯,噻吩,CuI,Paal-Knorr 合成介绍最近,我们报道了通过氰基乙酸甲酯与α,β-不饱和酮的共轭加成和随后的 CuI 介导的需氧氧化合成 2,5-二酮酯的有效方法。
2-Furancarboxylic acid hydrazides and pharmaceutical compositions containing the same
申请人:Fujii Akihito
公开号:US20050171196A1
公开(公告)日:2005-08-04
The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof, methods for producing them and pharmaceutical compositions containing them:
wherein A is a group represented by Formula (a) or the like:
(wherein either R
4
or R
5
represents cyano, nitro or the like, and the other represents a hydrogen atom or the like);
either R
1
or R
2
represents a group: -D-(X)m-R
6
or the like, and the other represents a group: -E-(Y)n-R
7
, hydrogen atom, aryl or the like;
R
3
is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like;
R
6
and R
7
independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted. Such compounds exhibit a potent antagonistic activity on glucagon receptor and are of use as preventive and/or therapeutic agents for symptoms and diseases in which glucagon is involved.
2-FURANCARBOXYLIC ACID HYDRAZIDES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
申请人:DAINIPPON PHARMACEUTICAL CO., LTD.
公开号:EP1489077A1
公开(公告)日:2004-12-22
The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula
(I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof, methods for producing them and pharmaceutical compositions containing them:
wherein A is a group represented by Formula (a) or the like:
(wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like);
either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like;
R3 is a hydrogen atom or the like;
D and E independently represent aryl;
X and Y independently represent 0 or the like;
R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and
m and n are independently 0 or 1, provided that the aryl is optionally substituted. Such compounds exhibit a potent antagonistic activity on glucagon receptor and are of use as preventive and/or therapeutic agents for symptoms and diseases in which glucagon is involved.
本发明提供由通式表示的 2-呋喃羧酸酰肼化合物
(I)代表的2-呋喃羧酸酰肼化合物及其原药、生理上可接受的盐、水合物、溶液,以及生产它们的方法和含有它们的药物组合物:
其中 A 是由式(a)代表的基团或类似基团:
(其中 R4 或 R5 代表氰基、硝基或类似物,另一个代表氢原子或类似物);
R1 或 R2 代表一个基团:-D-(X)m-R6 或类似基团,另一个代表一个基团:-E-(Y)n-R7、氢原子、芳基或类似基团;
R3 是氢原子或类似物;
D 和 E 各自代表芳基;
X 和 Y 独立地代表 0 或类似物;
R6 和 R7 独立地代表烷基、芳基、芳烷基或类似物;以及
m 和 n 独立地为 0 或 1,前提是芳基被任选取代。此类化合物对胰高血糖素受体具有强效的拮抗活性,可用作胰高血糖素相关症状和疾病的预防和/或治疗药物。
PIPERIDINE AND PIPERAZINE DERIVATIVES AS P2X3 ANTAGONISTS