Parallel Synthesis of 1,6-Disubstituted-1,2,4-triazin-3-ones on Solid-Phase

Autor:	Richard A. Houghten, Miao Hu, Wei Huang, Yongping Yu, Marc A. Giulianotti
Rok vydání:	2013
Předmět:	Triazines Chemistry Bioactive molecules Hydrazine Imidazoles General Chemistry General Medicine Borane Article MBHA resin chemistry.chemical_compound Hydrazines Cyclization Yield (chemistry) Phase (matter) Solid-Phase Synthesis Techniques Peptide bond Organic chemistry
Zdroj:	ACS Combinatorial Science. 15:335-339
ISSN:	2156-8944 2156-8952
Popis:	A parallel solid-phase synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones from MBHA resin is described. The reduction of resin-bound nitrosamino acids provides hydrazines efficiently without affecting the amide bond. The trityl protected hydrazine is then reduced with borane, and cyclized with 1,1-carbonyldiimidazole. The desired products are cleaved from their solid support and obtained in good yield and purity. This methodology is of value for the rapid parallel preparation of these potentially bioactive molecules.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3a16cb7af337044531f20d2e4361ce4 https://doi.org/10.1021/co400064d Zobrazit plný text záznamu