期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 4, 页码 941-945出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.12.005
关键词
CCR5 antagonist; HIV-1; antiviral; pyrazole
Modifications of the alkyl acetic acid portion and the phenyl on pyrrolidine in our lead pyrazole compound I afforded the isopropyl compound 9. This compound is a potent CCR5 antagonist showing good in vitro antiviral activity against HIV-1, an excellent selectivity profile, and good oral bioavailability in three animal species. During this investigation, a new method for the preparation of alpha-(pyrrolidin-1-yl)-alpha,alpha-dialkyl acetic acid from a pyrrolidine and alpha-bromo-alpha,alpha-dialkyl acetic acid using silver triflate was discovered. This allowed us to prepare compounds such as 24 and 25 for the first time. A novel Pd-mediated N-dealkylation of alpha-(pyrrolidin-1-yl)acetic acid was also uncovered. (C) 2004 Elsevier Ltd. All rights reserved.
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