681249-56-9Relevant articles and documents
Synthesis process of PARP inhibitor fluzopanb intermediate
-
Paragraph 0031-0032; 0037-0041; 0046-0050; 0054-0058; 0063, (2020/09/16)
The invention discloses a process method suitable for large-scale preparation of 2-trifluoromethyl [1,2,4]triazolo[1,5-a] pyrazine, and belongs to the field of drug intermediate synthesis, wherein 2-aminopyrazine and ethyl trifluoroacetate are used as raw materials, and a transesterification reaction, a substitution reaction and a dehydration reaction are performed to obtain 2-trifluoromethyl [1,2,4]triazolo[1,5-a] pyrazine. According to the process disclosed by the invention, cheap ethyl trifluoroacetate is selected to replace expensive trifluoroacetic anhydride, other organic solvents replace a first-class solvent dichloroethane, and TFFA replaces PPA which is difficult to post-treat, so that the production cost of existing biological, medical and chemical intermediates is greatly reduced, amplification verification is conducted on the kilogram-level scale of the process, the yield and the product purity are basically equivalent to those of the gram-level scale, and the process is expected to serve as an industrial large-scale production process.
AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
-
Page/Page column 33, (2008/06/13)
The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
FUSED TRIAZOLE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
-
Page/Page column 49, (2008/06/13)
The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.