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Items: 1 to 50 of 80

1.

Post-Synthetic Modification of Oligonucleotides via Orthogonal Amidation and Copper Catalyzed Cycloaddition Reactions.

Zewge D, Butora G, Sherer EC, Tellers DM, Sidler DR, Gouker J, Copeland G, Jadhav V, Li Z, Armstrong J, Davies IW.

Bioconjug Chem. 2018 Jun 20;29(6):1859-1865. doi: 10.1021/acs.bioconjchem.8b00298. Epub 2018 Jun 12.

PMID:
29893553
2.

Mapping the dark space of chemical reactions with extended nanomole synthesis and MALDI-TOF MS.

Lin S, Dikler S, Blincoe WD, Ferguson RD, Sheridan RP, Peng Z, Conway DV, Zawatzky K, Wang H, Cernak T, Davies IW, DiRocco DA, Sheng H, Welch CJ, Dreher SD.

Science. 2018 Aug 10;361(6402). pii: eaar6236. doi: 10.1126/science.aar6236. Epub 2018 May 24.

PMID:
29794218
3.

Beyond optical rotation: what's left is not always right in total synthesis.

Joyce LA, Nawrat CC, Sherer EC, Biba M, Brunskill A, Martin GE, Cohen RD, Davies IW.

Chem Sci. 2017 Oct 30;9(2):415-424. doi: 10.1039/c7sc04249c. eCollection 2018 Jan 14.

4.

Selective Hydrogen Atom Abstraction through Induced Bond Polarization: Direct α-Arylation of Alcohols through Photoredox, HAT, and Nickel Catalysis.

Twilton J, Christensen M, DiRocco DA, Ruck RT, Davies IW, MacMillan DWC.

Angew Chem Int Ed Engl. 2018 May 4;57(19):5369-5373. doi: 10.1002/anie.201800749. Epub 2018 Apr 6.

PMID:
29490112
5.

A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals.

Koniarczyk JL, Hesk D, Overgard A, Davies IW, McNally A.

J Am Chem Soc. 2018 Feb 14;140(6):1990-1993. doi: 10.1021/jacs.7b11710. Epub 2018 Feb 5.

PMID:
29377684
6.

Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds.

Loh YY, Nagao K, Hoover AJ, Hesk D, Rivera NR, Colletti SL, Davies IW, MacMillan DWC.

Science. 2017 Dec 1;358(6367):1182-1187. doi: 10.1126/science.aap9674. Epub 2017 Nov 9.

7.

Concise syntheses and HCV NS5B polymerase inhibition of (2'R)-3 and (2'S)-2'-ethynyluridine-10 and related nucleosides.

Bennett F, Buevich AV, Huang HC, Girijavallabhan V, Kerekes AD, Huang Y, Malikzay A, Smith E, Ferrari E, Senior M, Osterman R, Wang L, Wang J, Pu H, Truong QT, Tawa P, Bogen SL, Davies IW, Weber AE.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5349-5352. doi: 10.1016/j.bmcl.2017.06.064. Epub 2017 Jun 24.

PMID:
29056248
8.

Oxyfunctionalization of the Remote C-H Bonds of Aliphatic Amines by Decatungstate Photocatalysis.

Schultz DM, Lévesque F, DiRocco DA, Reibarkh M, Ji Y, Joyce LA, Dropinski JF, Sheng H, Sherry BD, Davies IW.

Angew Chem Int Ed Engl. 2017 Nov 27;56(48):15274-15278. doi: 10.1002/anie.201707537. Epub 2017 Oct 26.

PMID:
29044797
9.

A General Small-Scale Reactor To Enable Standardization and Acceleration of Photocatalytic Reactions.

Le CC, Wismer MK, Shi ZC, Zhang R, Conway DV, Li G, Vachal P, Davies IW, MacMillan DWC.

ACS Cent Sci. 2017 Jun 28;3(6):647-653. doi: 10.1021/acscentsci.7b00159. Epub 2017 May 17.

10.

A rational pre-catalyst design for bis-phosphine mono-oxide palladium catalyzed reactions.

Ji Y, Li H, Hyde AM, Chen Q, Belyk KM, Lexa KW, Yin J, Sherer EC, Williamson RT, Brunskill A, Ren S, Campeau LC, Davies IW, Ruck RT.

Chem Sci. 2017 Apr 1;8(4):2841-2851. doi: 10.1039/c6sc05472b. Epub 2017 Jan 19.

11.

A multifunctional catalyst that stereoselectively assembles prodrugs.

DiRocco DA, Ji Y, Sherer EC, Klapars A, Reibarkh M, Dropinski J, Mathew R, Maligres P, Hyde AM, Limanto J, Brunskill A, Ruck RT, Campeau LC, Davies IW.

Science. 2017 Apr 28;356(6336):426-430. doi: 10.1126/science.aam7936.

PMID:
28450641
12.

Design and Synthesis of P2-P4 Macrocycles Containing a Unique Spirocyclic Proline: A New Class of HCV NS3/4A Inhibitors.

Velázquez F, Chelliah M, Clasby M, Guo Z, Howe J, Miller R, Neelamkavil S, Shah U, Soriano A, Xia Y, Venkatraman S, Chackalamannil S, Davies IW.

ACS Med Chem Lett. 2016 Oct 17;7(12):1173-1178. eCollection 2016 Dec 8.

13.

MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.

Haidle AM, Childers KK, Zabierek AA, Katz JD, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Stanton MG, Davies IW, Munoz B, Northrup A.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):109-113. doi: 10.1016/j.bmcl.2016.08.066. Epub 2016 Aug 25.

PMID:
27894874
14.

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Katz JD, Haidle A, Childers KK, Zabierek AA, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Su HP, Munshi S, Stanton MG, Davies IW, Munoz B, Northrup A.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):114-120. doi: 10.1016/j.bmcl.2016.08.068. Epub 2016 Oct 22.

PMID:
27816515
15.

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.

Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA.

J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15.

16.

Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.

Tong L, Yu W, Coburn CA, Chen L, Selyutin O, Zeng Q, Dwyer MP, Nair AG, Shankar BB, Kim SH, Yang DY, Rosenblum SB, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Carr D, Curry S, McMonagle P, Bystol K, Lahser F, Ingravallo P, Chen S, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5354-5360. doi: 10.1016/j.bmcl.2016.08.097. Epub 2016 Sep 2.

PMID:
27680588
17.

Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents.

Greshock TJ, Moore KP, McClain RT, Bellomo A, Chung CK, Dreher SD, Kutchukian PS, Peng Z, Davies IW, Vachal P, Ellwart M, Manolikakes SM, Knochel P, Nantermet PG.

Angew Chem Int Ed Engl. 2016 Oct 24;55(44):13714-13718. doi: 10.1002/anie.201604652. Epub 2016 Sep 30.

PMID:
27690172
18.

Aryl amination using ligand-free Ni(II) salts and photoredox catalysis.

Corcoran EB, Pirnot MT, Lin S, Dreher SD, DiRocco DA, Davies IW, Buchwald SL, MacMillan DW.

Science. 2016 Jul 15;353(6296):279-83. doi: 10.1126/science.aag0209. Epub 2016 Jun 23.

19.

Chemistry informer libraries: a chemoinformatics enabled approach to evaluate and advance synthetic methods.

Kutchukian PS, Dropinski JF, Dykstra KD, Li B, DiRocco DA, Streckfuss EC, Campeau LC, Cernak T, Vachal P, Davies IW, Krska SW, Dreher SD.

Chem Sci. 2016 Apr 21;7(4):2604-2613. doi: 10.1039/c5sc04751j. Epub 2016 Jan 26.

20.

Discovery and mechanistic study of a photocatalytic indoline dehydrogenation for the synthesis of elbasvir.

Yayla HG, Peng F, Mangion IK, McLaughlin M, Campeau LC, Davies IW, DiRocco DA, Knowles RR.

Chem Sci. 2016 Mar 1;7(3):2066-2073. doi: 10.1039/c5sc03350k. Epub 2015 Dec 7.

21.

Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.

Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S.

ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14.

22.

P2Et Phosphazene: A Mild, Functional Group Tolerant Base for Soluble, Room Temperature Pd-Catalyzed C-N, C-O, and C-C Cross-Coupling Reactions.

Buitrago Santanilla A, Christensen M, Campeau LC, Davies IW, Dreher SD.

Org Lett. 2015 Jul 2;17(13):3370-3. doi: 10.1021/acs.orglett.5b01648. Epub 2015 Jun 22.

PMID:
26099020
23.

Organic chemistry. Nanomole-scale high-throughput chemistry for the synthesis of complex molecules.

Buitrago Santanilla A, Regalado EL, Pereira T, Shevlin M, Bateman K, Campeau LC, Schneeweis J, Berritt S, Shi ZC, Nantermet P, Liu Y, Helmy R, Welch CJ, Vachal P, Davies IW, Cernak T, Dreher SD.

Science. 2015 Jan 2;347(6217):49-53. doi: 10.1126/science.1259203. Epub 2014 Nov 20.

24.

High-throughput chemical modification of oligonucleotides for systematic structure-activity relationship evaluation.

Zewge D, Gosselin F, Kenski DM, Li J, Jadhav V, Yuan Y, Nerurkar SS, Tellers DM, Flanagan WM, Davies IW.

Bioconjug Chem. 2014 Dec 17;25(12):2222-32. doi: 10.1021/bc500453q. Epub 2014 Nov 21.

PMID:
25398098
25.

Cyclic-disulfide-based prodrugs for cytosol-specific drug delivery.

Butora G, Qi N, Fu W, Nguyen T, Huang HC, Davies IW.

Angew Chem Int Ed Engl. 2014 Dec 15;53(51):14046-50. doi: 10.1002/anie.201407130. Epub 2014 Oct 24.

PMID:
25346363
26.

Asymmetric hydrogenation of pyridinium salts with an iridium phosphole catalyst.

Chang M, Huang Y, Liu S, Chen Y, Krska SW, Davies IW, Zhang X.

Angew Chem Int Ed Engl. 2014 Nov 17;53(47):12761-4. doi: 10.1002/anie.201406762. Epub 2014 Oct 8.

PMID:
25297378
27.

Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.

Shah U, Jayne C, Chackalamannil S, Velázquez F, Guo Z, Buevich A, Howe JA, Chase R, Soriano A, Agrawal S, Rudd MT, McCauley JA, Liverton NJ, Romano J, Bush K, Coleman PJ, Grisé-Bard C, Brochu MC, Charron S, Aulakh V, Bachand B, Beaulieu P, Zaghdane H, Bhat S, Han Y, Vacca JP, Davies IW, Weber AE, Venkatraman S.

ACS Med Chem Lett. 2014 Jan 9;5(3):264-9. doi: 10.1021/ml400466p. eCollection 2014 Mar 13.

28.

Improving the in vivo therapeutic index of siRNA polymer conjugates through increasing pH responsiveness.

Guidry EN, Farand J, Soheili A, Parish CA, Kevin NJ, Pipik B, Calati KB, Ikemoto N, Waldman JH, Latham AH, Howell BJ, Leone A, Garbaccio RM, Barrett SE, Parmar RG, Truong QT, Mao B, Davies IW, Colletti SL, Sepp-Lorenzino L.

Bioconjug Chem. 2014 Feb 19;25(2):296-307. doi: 10.1021/bc400442p. Epub 2014 Jan 10.

PMID:
24409989
29.

siRNA-optimized Modifications for Enhanced In Vivo Activity.

Kenski DM, Butora G, Willingham AT, Cooper AJ, Fu W, Qi N, Soriano F, Davies IW, Flanagan WM.

Mol Ther Nucleic Acids. 2012 Jan 24;1:e5. doi: 10.1038/mtna.2011.4.

30.

Nucleoside optimization for RNAi: a high-throughput platform.

Butora G, Kenski DM, Cooper AJ, Fu W, Qi N, Li JJ, Flanagan WM, Davies IW.

J Am Chem Soc. 2011 Oct 26;133(42):16766-9. doi: 10.1021/ja2068774. Epub 2011 Sep 30.

PMID:
21942264
31.

Synthesis of vaniprevir (MK-7009): lactamization to prepare a 20-membered [corrected] macrocycle.

Song ZJ, Tellers DM, Journet M, Kuethe JT, Lieberman D, Humphrey G, Zhang F, Peng Z, Waters MS, Zewge D, Nolting A, Zhao D, Reamer RA, Dormer PG, Belyk KM, Davies IW, Devine PN, Tschaen DM.

J Org Chem. 2011 Oct 7;76(19):7804-15. doi: 10.1021/jo2011494. Epub 2011 Aug 31. Erratum in: J Org Chem. 2011 Nov 18;76(22):9553.

PMID:
21838271
32.

Preparative scale synthesis of the biaryl core of anacetrapib via a ruthenium-catalyzed direct arylation reaction: unexpected effect of solvent impurity on the arylation reaction.

Ouellet SG, Roy A, Molinaro C, Angelaud R, Marcoux JF, O'Shea PD, Davies IW.

J Org Chem. 2011 Mar 4;76(5):1436-9. doi: 10.1021/jo1018574. Epub 2011 Feb 1.

PMID:
21284400
33.

Practical synthesis of a renin inhibitor via a diastereoselective Dieckmann cyclization.

Gauvreau D, Hughes GJ, Lau SY, McKay DJ, O'Shea PD, Sidler RR, Yu B, Davies IW.

Org Lett. 2010 Nov 19;12(22):5146-9. doi: 10.1021/ol102131e. Epub 2010 Oct 14.

PMID:
20945851
34.

Controlled synthesis of 2- and 3-substituted benzo[b]furans.

Pei T, Chen CY, DiMichele L, Davies IW.

Org Lett. 2010 Nov 5;12(21):4972-5. doi: 10.1021/ol102123u.

PMID:
20873816
35.

Asymmetric hydrogenation of protected allylic amines.

Steinhuebel DP, Krska SW, Alorati A, Baxter JM, Belyk K, Bishop B, Palucki M, Sun Y, Davies IW.

Org Lett. 2010 Sep 17;12(18):4201-3. doi: 10.1021/ol101804e.

PMID:
20735080
36.

A practical synthesis of 5-lipoxygenase inhibitor MK-0633.

Gosselin F, Britton RA, Davies IW, Dolman SJ, Gauvreau D, Hoerrner RS, Hughes G, Janey J, Lau S, Molinaro C, Nadeau C, O'Shea PD, Palucki M, Sidler R.

J Org Chem. 2010 Jun 18;75(12):4154-60. doi: 10.1021/jo100561u.

PMID:
20486715
37.

Scalable synthesis of a prostaglandin EP4 receptor antagonist.

Gauvreau D, Dolman SJ, Hughes G, O'Shea PD, Davies IW.

J Org Chem. 2010 Jun 18;75(12):4078-85. doi: 10.1021/jo1004197.

PMID:
20469914
38.

A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285.

Gosselin F, Lau S, Nadeau C, Trinh T, O'Shea PD, Davies IW.

J Org Chem. 2009 Oct 16;74(20):7790-7. doi: 10.1021/jo901798d.

PMID:
19777997
39.

Looking forward in pharmaceutical process chemistry.

Davies IW, Welch CJ.

Science. 2009 Aug 7;325(5941):701-4. doi: 10.1126/science.1174501.

PMID:
19661417
40.

Enantioselective hydrogenation of N-H imines.

Hou G, Gosselin F, Li W, McWilliams JC, Sun Y, Weisel M, O'Shea PD, Chen CY, Davies IW, Zhang X.

J Am Chem Soc. 2009 Jul 29;131(29):9882-3. doi: 10.1021/ja903319r.

PMID:
19569686
41.

A general method for the synthesis of 3,5-diarylcyclopentenones via friedel-crafts acylation of vinyl chlorides.

Xu Y, McLaughlin M, Chen CY, Reamer RA, Dormer PG, Davies IW.

J Org Chem. 2009 Jul 17;74(14):5100-3. doi: 10.1021/jo900696k.

PMID:
19485346
42.

Palladium-catalyzed tandem Heck reaction/C-H functionalization--preparation of spiro-indane-oxindoles.

Ruck RT, Huffman MA, Kim MM, Shevlin M, Kandur WV, Davies IW.

Angew Chem Int Ed Engl. 2008;47(25):4711-4. doi: 10.1002/anie.200800549. No abstract available.

PMID:
18491340
43.

A simple, modular method for the synthesis of 3,4,5-trisubstituted pyrazoles.

McLaughlin M, Marcantonio K, Chen CY, Davies IW.

J Org Chem. 2008 Jun 6;73(11):4309-12. doi: 10.1021/jo800321p. Epub 2008 Apr 30.

PMID:
18444682
44.

Expanding the [1,2]-aryl migration to the synthesis of substituted indoles.

Pei T, Chen CY, Dormer PG, Davies IW.

Angew Chem Int Ed Engl. 2008;47(22):4231-3. doi: 10.1002/anie.200705804. No abstract available.

PMID:
18442144
45.

Raney-Co mediated reductive cyclization of an alpha,beta-unsaturated nitrile.

Janey JM, Orella CJ, Njolito E, Baxter JM, Rosen JD, Palucki M, Sidler RR, Li W, Kowal JJ, Davies IW.

J Org Chem. 2008 Apr 18;73(8):3212-7. doi: 10.1021/jo8000996. Epub 2008 Mar 19.

PMID:
18348575
46.

A general and efficient 2-amination of pyridines and quinolines.

Yin J, Xiang B, Huffman MA, Raab CE, Davies IW.

J Org Chem. 2007 Jun 8;72(12):4554-7. Epub 2007 May 15.

PMID:
17500567
47.

Magnesiation of electron-rich aryl bromides and their use in nickel-catalyzed cross-coupling reactions.

Lau SY, Hughes G, O'Shea PD, Davies IW.

Org Lett. 2007 May 24;9(11):2239-42. Epub 2007 May 5.

PMID:
17480092
48.

A practical synthesis of alpha-aryl methyl ketones via a transition-metal-free Meerwein arylation.

Molinaro C, Mowat J, Gosselin F, O'Shea PD, Marcoux JF, Angelaud R, Davies IW.

J Org Chem. 2007 Mar 2;72(5):1856-8. Epub 2007 Jan 31.

PMID:
17263583
49.

Superior reactivity of thiosemicarbazides in the synthesis of 2-amino-1,3,4-oxadiazoles.

Dolman SJ, Gosselin F, O'Shea PD, Davies IW.

J Org Chem. 2006 Dec 8;71(25):9548-51.

PMID:
17137395
50.

Stereoselective preparation of a cyclopentane-based NK1 receptor antagonist bearing an unsymmetrically substituted sec-sec ether.

Kuethe JT, Marcoux JF, Wong A, Wu J, Hillier MC, Dormer PG, Davies IW, Hughes DL.

J Org Chem. 2006 Sep 15;71(19):7378-90.

PMID:
16958533

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