14733-77-8, Name is 5-Amino-2,3-dihydro-1,3-benzoxazol-2-one, belongs to benzoxazole compound, is a common compound. Safety of 5-Amino-2,3-dihydro-1,3-benzoxazol-2-oneIn an article, once mentioned the new application about 14733-77-8.
Synthesis of the isotopically labeled JAK1/3 inhibitor [D7]-R545 and its oxidative metabolite [D7]-R935: Protecting group-directed regioselective bromination to access 3,4,5-substituted anilines
An extensive medicinal chemistry campaign and subsequent SAR studies led to the discovery of the highly potent and selective JAK1/3 inhibitor R545. To support advanced pre-clinical DMPK studies of R545, the isotopically labeled versions of the drug and its metabolite R935 were required. Herein, we describe the development of synthetic routes to deuterium-labeled [D7]-R545 and its oxidative metabolite [D7]-R935. Deuterium atoms were introduced at several sites in the target molecules by employing a convergent synthesis strategy. The desired regiochemistry at the right-hand side of [D7]-R935 was established via a newly discovered protecting group-directed bromination. The described synthetic approach gave rise to the desired deuterium-labeled target compounds and sufficient quantities were synthesized to enable pre-clinical DMPK studies.
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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem