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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: collins mr. 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.
A new reagent for direct difluoromethylation.
Fujiwara Y, Dixon JA, Rodriguez RA, Baxter RD, Dixon DD, Collins MR, Blackmond DG, Baran PS. Fujiwara Y, et al. Among authors: collins mr. J Am Chem Soc. 2012 Jan 25;134(3):1494-7. doi: 10.1021/ja211422g. Epub 2012 Jan 13. J Am Chem Soc. 2012. PMID: 22229949 Free PMC article.
Practical and innate carbon-hydrogen functionalization of heterocycles.
Fujiwara Y, Dixon JA, O'Hara F, Funder ED, Dixon DD, Rodriguez RA, Baxter RD, Herlé B, Sach N, Collins MR, Ishihara Y, Baran PS. Fujiwara Y, et al. Among authors: collins mr. Nature. 2012 Dec 6;492(7427):95-9. doi: 10.1038/nature11680. Epub 2012 Nov 28. Nature. 2012. PMID: 23201691 Free PMC article.
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: collins mr. 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.
A simple litmus test for aldehyde oxidase metabolism of heteroarenes.
O'Hara F, Burns AC, Collins MR, Dalvie D, Ornelas MA, Vaz AD, Fujiwara Y, Baran PS. O'Hara F, et al. Among authors: collins mr. J Med Chem. 2014 Feb 27;57(4):1616-20. doi: 10.1021/jm4017976. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24472070 Free PMC article.
C-H methylation of heteroarenes inspired by radical SAM methyl transferase.
Gui J, Zhou Q, Pan CM, Yabe Y, Burns AC, Collins MR, Ornelas MA, Ishihara Y, Baran PS. Gui J, et al. Among authors: collins mr. J Am Chem Soc. 2014 Apr 2;136(13):4853-6. doi: 10.1021/ja5007838. Epub 2014 Mar 21. J Am Chem Soc. 2014. PMID: 24611732 Free PMC article.
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. Johnson TW, et al. Among authors: collins mr. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116
Simple sulfinate synthesis enables C-H trifluoromethylcyclopropanation.
Gianatassio R, Kawamura S, Eprile CL, Foo K, Ge J, Burns AC, Collins MR, Baran PS. Gianatassio R, et al. Among authors: collins mr. Angew Chem Int Ed Engl. 2014 Sep 8;53(37):9851-5. doi: 10.1002/anie.201406622. Epub 2014 Aug 3. Angew Chem Int Ed Engl. 2014. PMID: 25088979 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: collins mr. Science. 2016 Jan 15;351(6270):241-6. doi: 10.1126/science.aad6252. Science. 2016. PMID: 26816372 Free PMC article.
61 results