Literature DB >> 19391593

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

Akin H Davulcu1, Douglas D McLeod, Jun Li, Kishta Katipally, Adam Littke, Wendel Doubleday, Zhongmin Xu, Cary W McConlogue, Chiajen J Lai, Margaret Gleeson, Mark 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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Year:  2009        PMID: 19391593     DOI: 10.1021/jo9003508

Source DB:  PubMed          Journal:  J Org Chem        ISSN: 0022-3263            Impact factor:   4.354


  4 in total

1.  Separation of mandelic acid and its derivatives with new immobilized cellulose chiral stationary phase.

Authors:  Jie Zhou; Qian Liu; Guang-Jun Fu; Zhen-Zhong Zhang
Journal:  J Zhejiang Univ Sci B       Date:  2013-07       Impact factor: 3.066

2.  Synthesis, Cytotoxic Analysis, and Molecular Docking Studies of Tetrazole Derivatives via N-Mannich Base Condensation as Potential Antimicrobials.

Authors:  Ashraf Atef Hatamleh; Dunia Al Farraj; Sarah Salah Al-Saif; SathishKumar Chidambaram; Surendrakumar Radhakrishnan; Idhayadhulla Akbar
Journal:  Drug Des Devel Ther       Date:  2020-10-23       Impact factor: 4.162

3.  Functionalization of Tetrazoles Bearing the Electrochemically Cleavable 1N-(6-Methylpyridyl-2-methyl) Protecting Group.

Authors:  Konstantinos Grammatoglou; Madara Da Rziņa; Aigars Jirgensons
Journal:  ACS Omega       Date:  2022-05-16

4.  3-(4-Bromo-phen-yl)-1-butyl-5-[1-(2-chloro-6-methyl-phen-yl)-1H-tetra-zol-5-yl]imidazolidine-2,4-dione.

Authors:  Gabriel B Hall; Federico Medda; Sue A Roberts; Christopher Hulme
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-06-15
  4 in total

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