1,2,4-oxadiazole derivatives as immunomodulators
AssigneeAurigene Discovery Technologies Limited
InventorsPottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
Life of this patent
Estimating the term…
Abstract
The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is: R1 represents −CH2OtBu or −CH(CH3)OtBu, R3 represents −CH2C(O)NHCPh3, −CH2CH2C(O)NHCPh3, −CH2C(O)OtBu, or −CH2CH2C(O)OtBu, and Aaa is an amino acid residue selected from Thr and Ser; wherein the C-terminus thereof is esterified, and wherein the hydroxy moiety of the side chain of Thr or Ser is substituted with tbutyl; the base is triethylamine; and the solvent is tetrahydrofuran.
Claims2
A method of making a compound according to the following scheme:
- wherein:
- R1 represents —CH2OtBu or —CH(CH3)OtBu;
- Aaa is an amino acid residue selected from Thr and Ser;
- wherein the C-terminus thereof is esterified, and wherein the hydroxy moiety of the side chain of Thr or Ser is substituted with t-butyl;
- R3 represents —CH2C(O)NHCPh3, —CH2CH2C(O)NHCPh3, —CH2C(O)OtBu, or —CH2CH2C(O)OtBu;
- the base is triethylamine;
- and
- the solvent is tetrahydrofuran.
Dependencies are inferred from the claim text.