Improved synthesis of N1-substituted orotic acid derivatives

Abstract

An improved method for the synthesis of N1-substituted orotic acid derivatives is reported. The method involves sequential incorporation of nitrogen atoms to the pyrimidine structure from simple starting materials and thus allows the synthesis of N1-substituted orotic acid derivatives with single 15N label at either N-1 or N-3.

Convenient synthesis of N1-substituted orotic acid derivatives

“…13 The reported synthesis of N1-substituted orotic acid derivatives is time-consuming and low-yielding (Scheme 1, the combined yield for the synthesis of 1-cyclohexylorotic acid is about 15%). 11,14–18 Furthermore, we have found that the purification of the final orotic acids can be difficult sometimes. In this Letter , we report a convenient and efficient synthesis of N1-substituted orotic acid derivatives from readily available starting material.…”