882769-94-0Relevant articles and documents
Scale-up synthesis of a TRPV1 antagonist featuring a facile thiazolo[5,4-d]pyrimidine formation
Liu, Jing,Fitzgerald, Anne E.,Lebsack, Alec D.,Mani, Neelakandha S.
scheme or table, p. 382 - 388 (2012/02/01)
An efficient and practical synthesis of a TRPV1 inhibitor bearing a thiazolo[5,4-d]pyrimidine core was developed. The initial synthesis was modified to facilitate acylation of 5-aminopyrimidine and subsequent thiazole formation. The synthesis features an efficient two-pot, five-step process for the construction of the thiazolo[5,4-d]pyrimidine ring. The new route is concise, chromatography-free, and amenable to large-scale preparation.