Process research and development for a tetrazole-based growth hormone secretagogue (GHS) pharmaceutical development candidate

…, J Li, K Katipally, A Littke, W Doubleday…

Index: Davulcu, Akin H.; McLeod, Douglas D.; Li, Jun; Katipally, Kishta; Littke, Adam; Doubleday, Wendel; Xu, Zhongmin; McConlogue, Cary W.; Lai, Chiajen J.; Gleeson, Margaret; Schwinden, Mark; Parsons Jr., Rodney L. Journal of Organic Chemistry, 2009 , vol. 74, # 11 p. 4068 - 4079

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Citation Number: 20

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 (ie, without isolation of ...