6398-06-7Relevant articles and documents
PROCESSES FOR PREPARATION OF (S)-TERT-BUTYL 4,5-DIAMINO-5-OXOPENTANOATE
-
Paragraph 00321; 00322, (2019/03/12)
Provided are processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate, or a salt, solvate, hydrate, enantiomer, mixture of enantiomers, or isotopologue thereof. Also provided are solid forms of various intermediates and products obtained from the processes.
Synthesis and anticonvulsant evaluation of a series of (R)- and (S)-N- Cbz-α-aminoglutarimide and succinimide
Park,Lee,Choi
, p. 1297 - 1302 (2007/10/03)
A series of (R)- and (S)-N-Cbz-α-aminoimides(1 and 2) were synthesized and were investigated their anticonvulsant activities in the MES and PTZ test, and determined the neurotoxicities. The most active compound among them was (S)-N-Cbz-α-amino-N-methyl glutarimide(1d) and the ED50 value in the MES test was 36.1 mg/kg and the ED50 value in the PTZ test was 12.5 mg/kg. In the rotorod test for neurotoxicity, the TD50 value was 62.5 mg/kg.
Synthesis of the Dolastatin Thiazole Amino Acid Component (gln)Thz
Holzapfel, Cedric W.,Pettit, George R.
, p. 2323 - 2327 (2007/10/02)
The new thiazole amino acid (gln)Thz, found to occur as one unit of the marine sea hare cyclic pentapeptide dolastin 3, has been synthesized from L-glutamic acid by the route 2 -> 10e.The synthesis of Z-L-isoglutamine (4) was improved by selective ammonolysis of anhydride 3 at -60 deg C.A variety of reaction conditions were found to cause complete racemization during the Hantzsch thiazole synthesis step (9 -> 10).Deuterium labeling experiments indicated loss of the chiral center prior to formation of the thiazole system and suggested an imine-enamine type equilibration involving intermediates A B (Scheme II).The N-benzyloxycarbonyl derivative (10d) of (gln)Thz was partially resolved by employing brucine.
