950600-21-2Relevant academic research and scientific papers
Development of a practical synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors
Pfefferkorn, Jeffrey A.,Bowles, Daniel M.,Kissel, William,Boyles, David C.,Choi, Chulho,Larsen, Scott D.,Song, Yuntao,Sun, Kuai-Lin,Miller, Steven R.,Trivedi, Bharat K.
, p. 8124 - 8134 (2008/02/08)
This paper describes the development of an efficient and scalable second generation synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors. Compound 1 was identified as part of a discovery program aimed at finding improved treatments for hypercholesterolemia. Herein, we describe an efficient synthesis of its highly functionalized pyrrole core followed by attachment of the 3,5-dihydroxyhexanoic acid side chain via ylide olefination chemistry.
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors
Pfefferkorn, Jeffrey A.,Song, Yuntao,Sun, Kuai-Lin,Miller, Steven R.,Trivedi, Bharat K.,Choi, Chulho,Sorenson, Roderick J.,Bratton, Larry D.,Unangst, Paul C.,Larsen, Scott D.,Poel, Toni-Jo,Cheng, Xue-Min,Lee, Chitase,Erasga, Noe,Auerbach, Bruce,Askew, Valerie,Dillon, Lisa,Hanselman, Jeffrey C.,Lin, Zhiwu,Lu, Gina,Robertson, Andrew,Olsen, Karl,Mertz, Thomas,Sekerke, Catherine,Pavlovsky, Alexander,Harris, Melissa S.,Bainbridge, Graeme,Caspers, Nicole,Chen, Huifen,Eberstadt, Matthias
, p. 4538 - 4544 (2008/02/12)
This manuscript describes the design and synthesis of a series of pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. Analogs were optimized using structure-based design and physical property considerations resulting i
