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1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long-sought-after mimetics for ortho/meta-substituted arenes.
Zhao JX, Chang YX, He C, Burke BJ, Collins MR, Del Bel M, Elleraas J, Gallego GM, Montgomery TP, Mousseau JJ, Nair SK, Perry MA, Spangler JE, Vantourout JC, Baran PS. Zhao JX, et al. Among authors: spangler je. Proc Natl Acad Sci U S A. 2021 Jul 13;118(28):e2108881118. doi: 10.1073/pnas.2108881118. Proc Natl Acad Sci U S A. 2021. PMID: 34244445 Free PMC article.
Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity.
Lopchuk JM, Fjelbye K, Kawamata Y, Malins LR, Pan CM, Gianatassio R, Wang J, Prieto L, Bradow J, Brandt TA, Collins MR, Elleraas J, Ewanicki J, Farrell W, Fadeyi OO, Gallego GM, Mousseau JJ, Oliver R, Sach NW, Smith JK, Spangler JE, Zhu H, Zhu J, Baran PS. Lopchuk JM, et al. Among authors: spangler je. J Am Chem Soc. 2017 Mar 1;139(8):3209-3226. doi: 10.1021/jacs.6b13229. Epub 2017 Feb 20. J Am Chem Soc. 2017. PMID: 28140573 Free PMC article.
Hindered dialkyl ether synthesis with electrogenerated carbocations.
Xiang J, Shang M, Kawamata Y, Lundberg H, Reisberg SH, Chen M, Mykhailiuk P, Beutner G, Collins MR, Davies A, Del Bel M, Gallego GM, Spangler JE, Starr J, Yang S, Blackmond DG, Baran PS. Xiang J, et al. Among authors: spangler je. Nature. 2019 Sep;573(7774):398-402. doi: 10.1038/s41586-019-1539-y. Epub 2019 Sep 9. Nature. 2019. PMID: 31501569 Free PMC article.
Organic chemistry. Strain-release amination.
Gianatassio R, Lopchuk JM, Wang J, Pan CM, Malins LR, Prieto L, Brandt TA, Collins MR, Gallego GM, Sach NW, Spangler JE, Zhu H, Zhu J, Baran PS. Gianatassio R, et al. Among authors: spangler je. Science. 2016 Jan 15;351(6270):241-6. doi: 10.1126/science.aad6252. Science. 2016. PMID: 26816372 Free PMC article.
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M. Kung PP, et al. J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27. J Med Chem. 2018. PMID: 29211475
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