A novel synthetic methodology for the preparation of Gemini Vitamin D3 analogues has been developed in this invention. These compounds are currently applied in the treatment of diverse diseases related with the lack of vitamin D. The efficient procedure involves a key chemical transformation (a sigmatropic rearrangement) that provides great versatility and selectivity in the synthesis of this type of compounds . Previous synthetic methods rely on the non-selective generation of the double side chain precursor and the subsequent separation of isomers. Besides, they often require the use of expensive and time-consuming chromatography techniques such as HPLC.
Commercial applications and Potential users:
Novel Gemini Vitamin D analogues can be of interest to the pharmaceutical industry as drug candidates for the treatment of diseases related with vitamin D deficiency.
State of art:
The synthesis has been performed at lab scale.
Publications:
- S. Tsuyako; O. Ryoko; H. Talin; O. James; U. Milan; M. Hubert; M. Stanislaw; J. Pawel; B. Riem; K. H Phillip Journal of Steroid Biochemistry and Molecular Biology 2008, 112, 151.
- S. J. Young; L. H. Jin; K. Amanda; P. Shiby; W. Chung-Xiou; M. Hubert; U. Milan; Z. Xi; C. Allan H; C. Li Molecular Pharmacology 2011, 79, 360.
Inventors:
Yagamare Fall Diop, Generosa Gómez Pacios, Manuel Pérez Vázquez, Zoila Gándara Barreiro, Xenxo Pérez García, Gonzalo Pazos Aguete, Guido Kurz.
Contacts:
Yagamare Fall Diop Organic Synthesis Research Group Phone: +34 986 812 320 yagamare@uvigo.es Oficina de I+D Tel. 986 812 236 Fax 986 812 140 webs.uvigo.es/otri/ otri@uvigo.es
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