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Aminocarbonylation of aryl tosylates to carboxamides.
Chung S, Sach N, Choi C, Yang X, Drozda SE, Singer RA, Wright SW. Chung S, et al. Org Lett. 2015 Jun 5;17(11):2848-51. doi: 10.1021/acs.orglett.5b01283. Epub 2015 May 21. Org Lett. 2015. PMID: 25994500
Synthesis of aryl ethers via a sulfonyl transfer reaction.
Sach NW, Richter DT, Cripps S, Tran-Dubé M, Zhu H, Huang B, Cui J, Sutton SC. Sach NW, et al. Org Lett. 2012 Aug 3;14(15):3886-9. doi: 10.1021/ol301615z. Epub 2012 Jul 17. Org Lett. 2012. PMID: 22799458
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP. Huang Q, et al. Among authors: sach nw. J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6. J Med Chem. 2014. PMID: 24432909 Free article.
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1 Receptor Inverse Agonist.
Lall MS, Bassyouni A, Bradow J, Brown M, Bundesmann M, Chen J, Ciszewski G, Hagen AE, Hyek D, Jenkinson S, Liu B, Obach RS, Pan S, Reilly U, Sach N, Smaltz DJ, Spracklin DK, Starr J, Wagenaar M, Walker GS. Lall MS, et al. J Med Chem. 2020 Jul 9;63(13):7268-7292. doi: 10.1021/acs.jmedchem.0c00483. Epub 2020 Jun 8. J Med Chem. 2020. PMID: 32462865
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222
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