Evaluation and Rapid Scale-Up of the Synthesis of the Pyrrolopyrimidines U-101033E and U-104067F

详细信息    查看全文

• 作者：Michael A. Mauragis ; Michael F. Veley ; and Michael F. Lipton
• 刊名：Organic Process Research & Development
• 出版年：1997
• 出版时间：January 1997
• 年：1997
• 卷：1
• 期：1
• 页码：39 - 44
• 全文大小：92K
• 年卷期：v.1,no.1(January 1997)
• ISSN：1520-586X

文摘

Large quantities of pure bulk drug were required toinitiatedevelopment for possible indications as antiasthma and neuroprotective agents. Safety concerns and reproducibilityproblems encountered with the laboratory procedures (Bundy, G.L.; et al. J. Med. Chem.1995, 38, 4161) forced thedevelopmentof a reliable large-scale process which within six monthsproduced >100 kg of U-104067 free base in a singlecampaign.During the course of this work, procedures were alsodevelopedwhich allowed for the bulk preparation of analyticallypure,pharmaceutically acceptable salt forms of both of thetitlecompounds.