Development of a Practical and Convergent Process for the Preparation of Sulopenem
摘要:
Previous synthetic processes for the preparation of sulopenem involved multistep linear sequences in which the chiral sulfoxide side chain was introduced early in the process. This contribution summarizes the development of a practical and convergent process for the large-scale preparation of 1. The key step in the synthesis involves cyclization of an oxalimide intermediate to provide the thiopenem core. This convergent strategy allows for late introduction of the expensive and labile chiral sulfoxide subunit. Additionally, a regioselective sulfur oxidation and an improved deprotection sequence were developed. The latter provides API of high purity without the need for recrystallization.
NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
申请人:Ryono Denis E.
公开号:US20080009465A1
公开(公告)日:2008-01-10
Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure
wherein
is a heteroaryl ring;
R
4
is —(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
), —(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
, —(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
, —(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10
), or —(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10
);
R
5
and R
6
are independently selected from H, alkyl and halogen;
Y is R
7
(CH
2
)
s
or is absent; and
X, n, Z, m, R
4
, R
5
, R
6
, R
7
, and s are as defined herein; or a pharmaceutically acceptable salt thereof.
A method for treating diabetes and related diseases employing the above compounds is also provided.
提供了磷酸酯和磷酸酯激活剂,因此在治疗糖尿病和相关疾病方面非常有用,并具有以下结构:
其中
是杂环芳基环;
R
4
为—(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
)、—(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
、—(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
、—(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10)
或—(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10)
;
R
5
和R
6
分别选择自H、烷基和卤素;
Y为R
7
(CH
2
)
s
或不存在;以及
X、n、Z、m、R
4
、R
5
、R
6
、R
7
和s如本文所定义;或其药用盐。
还提供了一种利用上述化合物治疗糖尿病和相关疾病的方法。
Metal‐Free Synthesis of
<i>N</i>
‐Aryl Amides using Organocatalytic Ring‐Opening Aminolysis of Lactones
作者:Wusheng Guo、José Enrique Gómez、Luis Martínez‐Rodríguez、Nuno A. G. Bandeira、Carles Bo、Arjan W. Kleij
DOI:10.1002/cssc.201700415
日期:2017.5.9
Catalytic ring‐opening of bio‐sourced non‐strained lactones with aromatic amines can offer a straightforward, 100 % atom‐economical, and sustainable pathway towards relevant N‐aryl amide scaffolds. Herein, the first general, metal‐free, and highly efficient N‐aryl amide formation is reported from poorly reactive aromatic amines and non‐strained lactones under mild operating conditions using an organic
Esters of ureido-phenyl (or pyridyl) phosphinic acids
申请人:Zoecon Corporation
公开号:US04433149A1
公开(公告)日:1984-02-21
Substituted tetrahydrobenzodiazaphosphorindiones or tetrahydropyridodiazaphosphorindiones, intermediates therefore, synthesis thereof, said compounds being useful herbicides.
Substituted tetrahydrobenzodiazaphosphorindiones or tetrahydropyridodiazaphosphorindiones, intermediates therefore, synthesis thereof, said compounds being useful herbicides.
The present application provides for a compound of Formula I or II:
or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.