Process Research and Development for a Tetrazole-Based Growth Hormone Secretagogue (GHS) Pharmaceutical Development Candidate
The Journal of Organic Chemistry2009Vol. 74(11), pp. 4068–4079
Citations Over TimeTop 19% of 2009 papers
Akin H. Davulcu, Douglas D. McLeod, Jun Li, Kishta Katipally, Adam F. Littke, Wendel W. Doubleday, Zhongmin Xu, Cary W. McConlogue, Chiajen Lai, Margaret Gleeson, Mark D. Schwinden, Rodney L. Parsons
Abstract
BMS-317180 (1) is a potent, orally active agonist of the human growth hormone secretagogue (GHS) receptor. This manuscript details the process research and development efforts that enabled the synthesis of the phosphate salt of 1 on a multi-kilogram scale. Key considerations in the development of this process focused on safe execution and the requirement for telescoped synthetic transformations (i.e., without isolation of intermediate products) to contend with a lack of suitably crystalline products.
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