Synthesis of paricalcitol: A novel strategy combining chemical and microbial transformations

Resumo

A novel strategy was developed for the preparation of paricalcitol (1α,25-dihydroxy-19-norvitamin D₂) via seven-step chemical transformation and one-step microbial transformation. Using vitamin D₂ as a starting material, 1α- and 25-hydroxyl groups of paricalcitol were introduced by Pseudonocardia autotrophica CGMCC5098 at the late stage of the synthesis, allowing us to avoid harsh reaction conditions and tedious steps. The overall yield of paricalcitol was 0.75%.