Process Research and Development for a Tetrazole-Based Growth Hormone Secretagogue (GHS) Pharmaceutical Development Candidate

IF 3.3 2区化学 Q1 CHEMISTRY, ORGANIC

Journal of Organic Chemistry Pub Date : 2009-04-24 DOI:10.1021/jo9003508

Akin H. Davulcu*, 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 Jr., *

引用次数: 31

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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基于四氮唑的生长激素分泌剂(GHS)候选药物的工艺研究与开发

BMS-317180(1)是一种有效的口服人类生长激素分泌剂(GHS)受体激动剂。这篇手稿详细介绍了过程研究和开发工作，使合成的磷酸盐1在数公斤规模。开发该工艺的关键考虑因素集中在安全执行和伸缩合成转化(即不隔离中间产品)的要求上，以应对缺乏适当结晶产品的问题。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Organic Chemistry 化学-有机化学

CiteScore

6.20

自引率

11.10%

发文量

1467

审稿时长

2 months

期刊介绍： Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.