114997-92-1

Upstream product

• 93794-41-3 2-mercaptobenzo[d]oxazole-5-carbonitrile 
• 93794-41-3 5-cyanobenzo[d]oxazole-2-(3H)-thiazone 
• 767-00-0 4-cyanophenol 
• 14543-43-2 3-amino-4-hydroxybenzonitrile 
• 3272-08-0 4-hydroxy-3-nitrobenzonitrile 

Downstream Products

• 613289-35-3 2-(5-acetoxyamidinobenzoxazol-2-yl)-5-(4-acetoxyamidinophenyl)furan 
• 613289-34-2 2-(5-hydroxyamidinobenzoxazol-2-yl)-5-(4-hydroxyamidinophenyl)furan 
• 613289-39-7 2-(5-cyanobenzoxazol-2-yl)-5-(4-cyanophenyl)thiophene 
• 613289-41-1 2-(5-cyanobenzoxazol-2-yl)-5-(4-cyanophenyl)furan 

Relevant academic research and scientific papers

Preparation method of benzo[d]oxazole derivative

The invention discloses a preparation method of a benzo[d]oxazole derivative, namely 2-chlorobenzo[d]oxazole-5-formamide. With 2-nitro-4-cyanophenol being an initial raw material, the target product is obtained through reducing, ring closure, chlorinating

BENZOTHIAZOLES HAVING HISTAMINE H3 RECEPTOR ACTIVITY

Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (l): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

PROLINE DERIVATIVES AND USE THEREOF AS DRUGS

The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

Facile rearrangements of alkynylamino heterocycles with noble metal cations

A number of 2-(alkynylamino)-substituted heterocycles have been synthesized. These heterocycles rearrange in the presence of silver(I) and gold(I) salts to give novel 2H-pyrimido[2,1-b]benzoxazoles, 2H-pyrimido[2,1-b]benzothiazoles, and a 2H-pyrimido[2,1-b]benzoselenazole. Two of the the 2H-pyrimido[2,1-b]benzoxazoles were isolated in good yield. The kinetics of the silver tetrafluoroborate-catalyzed rearrangements of selected (alkynylamino)benzoxazoles and benzothiazoles have been examined by 1H NMR in CD3CN. Factors affecting the electron densities of the triple bond and of the nitrogen atom in the heterocycle are important in influencing the rate of rearrangement.

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: Inhibitors of immune complex induced inflammation

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.