کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5227161 | 1383597 | 2009 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of two synthetic routes to CE-178,253, a CB1 antagonist for the treatment of obesity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
CE-178,253 benzenesulfonate (1) is a CB1 antagonist discovered by Pfizer medicinal chemists. Two syntheses of this compound are described. The first, based on the discovery synthesis, involves assembly of an aryl-substituted pyrazolotriazine core onto which the second aryl moiety is installed by a Suzuki coupling; this route has been scaled to provide up to 6Â kg of API. A second, more convergent route is also described, which installs the pyrazolotriazine containing both aryl substituents by condensation of a bromoketone with a substituted thiosemicarbazide. This route has been demonstrated on laboratory scale and is viewed as the preferred bond-forming sequence.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Tetrahedron - Volume 65, Issue 16, 18 April 2009, Pages 3292-3304
Journal: Tetrahedron - Volume 65, Issue 16, 18 April 2009, Pages 3292-3304
نویسندگان
Thomas A. Brandt, Stéphane Caron, David B. Damon, Joseph DiBrino, Arun Ghosh, David A. Griffith, Sandeep Kedia, John A. Ragan, Peter R. Rose, Brian C. Vanderplas, Lulin Wei,