Progress in Synthesis of hydrocortisone.docVIP

 PAGE \* MERGEFORMAT 25 Progress in Synthesis of hydrocortisone Author: Jia Chunyan Chen Jianxin Qiu-Xiang Yin Jing-Kang Wang [Abstract] Hydrocortisone is the major mammalian adrenal cortex hormones drugs and an important intermediate of steroidal drug synthesis. This paper provides a brief overview of its total chemical synthesis, semi-synthetic method and the whole bio-synthesis methods, the path of domestic and foreign situation and the related progress and direction of its development have been reviewed and prospects. [Keywords:] Hydrocortisone; steroidal drugs; chemical synthesis; semi-synthetic method; Biosynthesis ABSTRACT Hydrocortisone is the major glucocorticoid and an important intermediate in steroid drug synthesis. The main synthetic approaches and progresses including total chemical synthesis, semi-synthesis and whole-cell bioconversion for hydrocortisone manufacture in domestic and other countries were briefly reviewed. Prospective and evaluation of hydrocortisone synthesis were also discussed. KEY WORDS Hydrocortisone; Steroid agents; Chemical synthesis; Semi-synthesis; biosynthesis Hydrocortisone (hydrocortisone, HC) The chemical name is 11β , 17α , 21 - trihydroxy-pregnane -4 - ene -3,20 - dione, an adrenal cortical hormone medicines, is a hormone drugs, the largest output species, its structure shown in Figure 1. At present, China, Britain, the United States, Japan, France and other countries and the European Pharmacopoeia are close set. 5 body of HC is the major mammalian adrenal cortex to secrete glucocorticoids, their pharmacological effects through the dispersion in the target cells, and their receptors, the formation of steroid - receptor complex, activation of steroid - receptor complex as gene activation of transcription factors in the form of dimer and DNA sequence of chains on the specific combination of regulation of gene transcription, increase mRNA generation, and use it as the template synthesis of the corresponding Figure