Microwave assisted stereospecific synthesis of (S)-3-substituted 2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-diones
作者:Suresh K Pandey、Keshav K Awasthi、Anil K Saxena
DOI:10.1016/s0040-4020(01)00334-9
日期:2001.5
A new easy way of preparing (S)-3-substituted 2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-diones, an important intermediate compound, is described using microwave irradiation supported on silica gel. The reaction is generalised and good to excellent yields of enantiomerically pure products are obtained.
一种制备(S)-3-取代的2,3,6,7,12,12a-六氢吡嗪并[1',2':1,6]吡啶[3,4- b ]吲哚-1,4的简便方法使用载于硅胶上的微波辐射描述了重要的中间体化合物-二酮。反应被普遍进行,并且获得对映体纯产物的良好至极好的收率。
The present invention aims to provide an immunostimulating agent superior in an immunostimulatory effect, particularly a compound useful as a vaccine adjuvant, a pharmaceutical composition containing the compound, a vaccine containing the compound and an antigen.
An immunostimulating agent containing at least one kind of a compound represented by the formula (I):
wherein each symbol is as defined in the present specification, or a salt thereof.
1,3-Diarylprop-2-en-1-ones, compositions containing them and use thereof
申请人:AVENTIS PHARMA S.A.
公开号:US20030153611A1
公开(公告)日:2003-08-14
1,3-Diarylprop-2-en-1-ones and derivatives, compositions containing them, manufacturing process and use. Substituted 1,3-diarylprop-2-en-1-ones with therapeutic activity may be used in oncology.
Compound selected from those of formula (I):
1
wherein
2
represents an optionally substituted 5-membered nitrogen-containing heterocycle,
Ak represents an alkylene chain,
X represents a single bond or phenylene,
R
1
and R
2
, which may be identical or different, each represent hydrogen or alkyl,
R
3
represents alkyl, nitro or cyano,
Y represents NR
4
or CHNO
2
,
R
4
represents hydrogen or alkyl,
its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid,
with the exclusion of compounds wherein, simultaneously,
3
represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH
2
)
3
—, X represents a single bond, Y represents NH and R
3
represents nitro.
Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.