60567-47-7

Upstream product

• 850130-96-0 2-(4-methoxyphenyl)-1-(nitromethyl)-1,2,3,4-tetrahydroisoquinoline 
• 40615-08-5 [(isoquinolin-1-yl)methyl]amine 
• 1198-30-7 1-isoquinolinecarbonitrile 
• 78317-83-6 2-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline 
• 1447933-71-2 1-(R)-(N-cyclohexylcarboxamidomethyl)-2-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline 
• 91-21-4 1,2,3,4-tetrahydroisoquinoline 
• 1447933-67-6 1-(R)-(aminomethyl)-2-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline 
• 1132765-82-2 1-(aminomethyl)-2-(4-methoxyphenyl)-1,2,3,4-tetrahydroisoquinoline 

Downstream Products

• 57452-97-8 (+)-Praziquantel 

Relevant academic research and scientific papers

METHOD FOR THE PRODUCTION OF PRAZIQUANTEL AND PRECURSORS THEREOF

The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound (I) and subsequent cyclization.

Enhancing the usefulness of cross dehydrogenative coupling reactions with a removable protecting group

A removable protecting group has been identified that allows the products of widely-used cross dehydrogenative couplings to be synthetically elaborated. The method can be used with enantiopure amines with no loss of enantiomeric excess. The methodology is exemplified by a new synthesis of enantiopure praziquantel, the drug used in the treatment of millions of people suffering from the neglected tropical disease, schistosomiasis.